Publikationen von Prof. Dr. Oliver Werz

2024
Broos J.Y., van der Burgt R.T.M., Konings J., Rijnsburger M., Werz O., de Vries H.E., Giera M., Kooij G. (2024) Arachidonic acid-derived lipid mediators in multiple sclerosis pathogenesis: fueling or dampening disease progression?" J Neuroinflamm, 21:21

Cerchia C., Küfner L., Werz O.*, Lavecchia A.* (2024) Identification of selective 5-LOX and FLAP inhibitors as novel anti-inflammatory agents by ligand-based virtual screening. Eur J Med Chem, 263:115932

Schimanski J., Gresnigt M.S., Brunner E., Werz O., Hube B., Garscha U. (2024) Hyphal-associated protein expression is crucial for Candida albicans-induced eicosanoid biosynthesis in immune cells. Eur J Immunol, 17:e2350743

Nischang V., Witt F.M., Börner F., Gomez M., Jordan P.M., Werz O. (2024) Frankincense preparation promotes formation of inflammation-resolving lipid mediators by manipulating lipoxygenases in human innate immune cells. Front Pharmacol. 2024 Jan 4;14:1332628

Jordan P.M., Günther K., Nischang V., Ning Y., Deinhardt-Emmer S., Ehrhardt C., Werz O. (2024) Influenza A virus selectively elevates prostaglandin E2 formation in pro-resolving macrophages. iScience 27(1):108775

Ismail J., Klepsch L.C., Dahlke P., Tsarenko E., Vollrath A., Pretzel D., Jordan P.M., Rezaei K., Czaplewska J.A., Stumpf S., Beringer-Siemers B., Nischang I., Hoeppener S., Werz O., Schubert U.S. (2024) PEG-Lipid-PLGA Hybrid Particles for Targeted Delivery of Anti-Inflammatory Drugs. Pharmaceutics.16(2):187

Sharifi S., Chaudhari P., Martirosyan A., Eberhardt A.O., Witt F., Gollowitzer A., Lange L., Woitzat Y., Okoli E.M., Li H., Rahnis N., Kirkpatrick J., Werz O., Ori A., Koeberle A., Bierhoff H., Ermolaeva M. (2024) Reducing the metabolic burden of rRNA synthesis promotes healthy longevity in Caenorhabditis elegans. Nat Commun. 15(1):1702

Roman D., Meisinger P., Guillonneau R., Peng C.-C., Peltner L. K., Jordan P. M., Haensch V., Götze S., Werz O., Hertweck C., Chen Y., Beemelmanns C. (2024) Isolation and Total Synthesis Structure Revision of a Widespread Marine Cysteinolic acid-containing Sulfonolipid Class Based on their Isolation and Total Synthesis. Angew Chem, in press

Zahel P., Bruggink V., Hülsmann J., Steiniger F., Hofstetter R.K., Heinzel T., Beekmann U., Werz O., Kralisch D. (2024) Exploring Microemulsion Systems for the Incorporation of Glucocorticoids into Bacterial Cellulose: A Novel Approach for Anti-Inflammatory Wound Dressings. Pharmaceutics, in press.

Werz O., Stettler H., Theurer C., Seibel J. (2024) 125^th Anniversary of Aspirin - The Story Continues. Pharmaceuticals, in press

Speckmann B, Wagner T, Jordan PM, Werz O, Wilhelm M, Tom Dieck H, Schön C. (2024) Synbiotic Bacillus megaterium DSM 32963 and n-3 PUFA Salt Composition Elevates Pro-Resolving Lipid Mediator Levels in Healthy Subjects: A Randomized Controlled Study. Nutrients. 2024;16(9):1354

Gür Maz T., Dahlke P., Ergül A.G., Olğaç A., Jordan P.M., Çalışkan B., Werz O., Banoglu E. (2024) Novel 1,3,4-oxadiazole derivatives as highly potent microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors. Bioorg. Chem., 147:107383

Gazzillo E., Colarusso E., Giordano A., Chini M.G., Potenza M., Hofstetter R.K., Iorizzi M., Werz O., Lauro G., Bifulco G. (2024) Repositioning of Small Molecules through the Inverse Virtual Screening in silico Tool: Case of Benzothiazole-Based Inhibitors of Soluble Epoxide Hydrolase (sEH). Chempluschem. 2024: e202400234.

Pace S., Meyer K.P.L., Troisi F., Bilancia R., D'Avino D., Parisi O., Rizza R., Stiuso P., Gerstmeier J., Schädel P., Ialenti A., Sautebin L., Serhan C.N., Rossi A., Borrelli F., Werz O. (2024) Sex hormone deprivation abolishes sex-specific differences in murine colon inflammation and related lipid mediator production. FASEB J. 31;38(14):e23828.

Bachmann V., Schädel P., Westhoff J., Perić M., Schömberg F., Skaltsounis A.L., Höppener S., Pantsar T., Fischer D., Vilotijević I., Werz O. (2024) Bromo-substituted indirubins for inhibition of protein kinase-mediated signalling involved in inflammatory mediator release in human monocytes. Bioorg. Chem. 2024;149:107470.

Günther K., Ehrhardt C., Werz O., Jordan P.M. (2024) Lipid mediator profiling and phenotyping of human M1- and M2-monocyte-derived macrophages during host-pathogen interactions. STAR Protoc, in press

Schultz C., Wegner T., Heusel C., Gallagher T., Zheng Y., Werner M., Wegner S.V.,Meyer-Zedler T., Werz O., Schmitt M., Popp J., Glorius F. (2024) Alkyne-tagged imidazolium-based membrane cholesterol analogs for Raman imaging applications. Chem. Sci., in press

Deng Y., Yu R., Grabe V., Sommermann T., Werner M., Vallet M., Zerfaß C., Werz O., Pohnert G. (2024) Bacteria modulate aging physiology in microalgae via induced vesicle production and the methionine cycle. Nat. Microbiol., in press

Barbari R., Bruggink V., Hofstetter R.K., Tupini C., Fagnani S., Baldini E., Durini E., Lampronti I., Vertuani S., Baldisserotto A.*, Werz O.,* Manfredini S. (2024) Synthesis and biological activity assessment of 2-styrylbenzothiazoles as potential multifunctional therapeutic agents. Antioxidants, 13(10):1196

Dörner S., Trottmann F., Jordan P.M., Rogge K., Bartels B., Werz O., Hertweck C., Hoffmeister D. (2024) The Fatal Mushroom Neurotoxin Muscarine is Released from a Harmless Phosphorylated Precursor upon Cellular Injury. Angew. Chem. Int. Ed. Engl., e202417220.

Tsarenko E., Göppert N.E., Dahlke P., Behnke M., Gangapurwala G., Beringer-Siemers B., Jaepel L., Kellner C., Pretzel D., Czaplewska J.A., Vollrath A., Jordan P.M., Weber C., Werz O., Schubert U.S., Nischang I. (2024) Unveiling the power of liquid chromatography in examining a library of degradable poly(2-oxazoline)s in nanomedicine applications. J Mat. Chem. B, in press

Ergül A.G., Jordan P.M., Dahlke P., Nur B., Olgac A., Uludağ O., Werz O.*, Çalışkan B.*, Banoglu E.* (2024) Novel Benzimidazole Derivatives as Potent Inhibitors of Microsomal Prostaglandin E2 Synthase 1 for the Potential Treatment of Inflammation, Pain, and Fever. J Med Chem, in press

Morgner B., WerzO., Wiegand C., Tittelbach J. (2024) Bilayered skin equivalent mimicking psoriasis as predictive tool for preclinical treatment studies, Commun. Biol., 7(1):1529.
2023
Werz O. (2023) Introduction to the lipid mediators special issue. Biochem Pharmacol. 207:115375

Lanas A., Werz O., Mikhai E. (2023) Comparison of gastrointestinal adverse events between fast release tablets and regular acetylsalicylic acid (aspirin) galenics after short-term use: A meta-analysis of randomized clinical trials. Inflammopharmacol, 31(5):2369-2381

Patrignani P., Schebb N.H., Werz O., Steinhilber D. (2023) Editorial: Lipidomics of Oxylipins in Biological Systems. Front Pharmacol, 14:1342596

Gur Maz T., Koc B., Jordan P.M., İbiş K., Çalışkan B., Werz O., Banoglu E. (2023) Benzoxazolone-5-urea Derivatives as Human Soluble Epoxide Hydrolase (sEH) Inhibitors, ACS Omega, 8(2):2445-2454

Börner F., Pace S., Jordan P.M., Gerstmeier J., Gomez M., Rossi A., Gilbert N.C., Newcomer M.E., Werz O. (2023) Allosteric activation of 15-lipoxygenase-1 by boswellic acid induces the lipid mediator class switch to promote resolution of inflammation. Adv Sci, 10(6):e2205604

Schwarz M., Löser A., Cheng Q., Wichmann-Costaganna M., Schädel P., Werz O., Arnér E.S.J., Kipp A.P. (2023) Side-by-side comparison of recombinant human glutathione peroxidases identifies overlapping substrate specificities for soluble hydroperoxides. Redox Biol, 59:102593

Naumann M., Arend N., Guliev R.R., Kretzer C., Rubio I., Werz O., Neugebauer U. (2023) Label-free characterization of macrophage polarization using Raman spectroscopy. Int J Mol Sci, 24(1), 824

Masi F., Chianese G., Hofstetter R.K., Cavallaro A.L., Werz O., Taglialatela-Scafatia O. (2023) Phytochemical profile and anti-inflammatory activity of a commercially available Rhodiola rosea root extract. Fitoterapia, 166, 105439

Behnke M, Klemm P, Dahlke P, Shkodra B, Beringer-Siemers B, Czaplewska JA, Stumpf S, Jordan PM, Schubert S, Hoeppener S, Vollrath A, Werz O, Schubert US (2023) Ethoxy acetalated dextran nanoparticles for drug delivery: A comparative study of formulation methods. Int J Pharm X, 5,100173.

Schädel P., Czapka A., Gebert N., Jacobsen I.D., Ori A., Werz O., Metabololipidomic and proteomic profiling reveals aberrant macrophage activation and interrelated immunomodulatory mediator release during aging. Aging Cell, 22(7), e13856

Röhrl J., Piqué-Borràs M.R., Jaklin M., Werner M., Werz O., Josef H., Hölz H., Ammendola A., Künstle G. (2023) Anti-Inflammatory Activities of Arnica montana Planta Tota versus Flower Extracts: Analytical, In Vitro and In Vivo Mouse Paw Oedema Model Studies. Plants 12(6),1348.

Teder T., König S., Singh R., Samuelsson B., Werz O., Garscha U., Haeggström J.Z. (2023) Modulation of the 5-lipoxgenase pathway by chalcogen-containing inhibitors of leukotriene A4 hydrolase. Int. J. Mol Sci., 24, 7539

Ning Y., Wang W., Jordan P.M., Barth S.A., Hofstetter R.K., Xu J., Zhang X., Cai Y., Menge C., Chen X., Werz O. (2023) Mycobacterium tuberculosis-Induced Prostaglandin J2 and 15-Deoxy-Prostaglandin J2 Inhibit Inflammatory Signals in Human M1 Macrophages via a Negative Feedback Loop. J. Immunol., 210, 1564-1575

Liao S., Gollowitzer A., Börmel L., Maier C., Gottschalk L., Werz O., Wallert M., Koeberle A., Lorkowski S. (2023) α-Tocopherol-13′-Carboxychromanol Induces Cell Cycle Arrest and Cell Death by Inhibiting the SREBP1-SCD1 Axis and Causing Imbalance in Lipid Desaturation. Int. J. Mol Sci. 24, 9229.

Liu X., Wenisch D., Dahlke P., Jordan P. M., Jakupec M.A., Kowol C.R., Liebing P., Werz O.*, Keppler B.K.*, Weigand W.* (2023) Multi-action platinum(IV) prodrugs conjugated with COX-inhibiting NSAIDs. Eur J Med Chem, 57, 115515

Musella S., D’Avino D., Peltner L.K., Di Sarno V., Cerqua I., Merciai F., Vestuto V., Ciaglia T., Smaldone G., Di Matteo F., Di Micco S., Napolitano V., Bifulco G., Pepe G., Sommella E., Basilicata M.G., Aquino G., Gomez-Monterrey I.M., Campiglia T., Ostacolo C., Roviezzo F., Werz O., Rossi A., Bertamino A. (2023) Design, synthesis and pharmacological characterization of a potent soluble epoxide hydrolase inhibitor for the treatment of acute pancreatitis. J Med Chem, 66(13):9201-9222

Schoenthaler M., Waltl L., Hasenoehrl T., Seher D., Lutz A., Aulinger L., Temml V., König S., Siller A., Braun D.E., Garscha U., Werz O., Schuster D., Schennach H, Koeberle A, Matuszczak B. (2023) Novel thiazolopyridine derivatives of diflapolin as dual sEH/FLAP inhibitors with improved solubility. Bioorg Chem, 139:106685

Rao Z, Brunner E, Giszas B, Iyer-Bierhoff A, Gerstmeier J, Börner F, Jordan PM, Pace S, Meyer KPL, Hofstetter RK, Merk D, Paulenz C, Heinzel T, Grunert PC, Stallmach A, Serhan CN, Werner M, Werz O. (2023) Glucocorticoids regulate lipid mediator networks by reciprocal modulation of 15-lipoxygenase isoforms affecting inflammation resolution. Proc. Natl. Acad. Sci. USA, 120(35):e2302070120

Olgac A., Çapan I., Dahlke P., Jordan P.M., Werz O., Banoglu E. (2023) Substituted 1,2,4-triazoles as novel and selective inhibitors of leukotriene biosynthesis targeting 5-lipoxygenase-activating protein (FLAP). ACS Omega, 8(34):31293-31304

Riedl R., Kühn A., Rietz D., Hebecker B., Glowalla K.-G., Peltner L.K., Jordan P.M., Werz O., Lorkowski S., Wiegand C., Wallert M. (2023) Establishment and Characterization of Mild Atopic Dermatitis in the DNCB-Induced Mouse Model. Int. J. Mol. Sci., 24(15):12325

Peltner L., Gluthmann L., Börner F., Pace S., Hoffstetter R.K., Kretzer C., Bilancia R., Pollastro F., Koeberle A., Appendino G., Rossi A., Newcomer M.E., Gilbert N.C., Werz O.*, Jordan P.M.* (2023) Cannabidiol acts as molecular switch in innate immune cells to promote the biosynthesis of inflammation-resolving lipid mediators. Cell Chem. Biol., 30(12):1508-1524

Jovičić E.J., Pucer Jane A., Eichmann T.O., Koren S., Brglez V., Jordan P.M., Gerstmeier J., Lainšček D., Golob-Urbanc A., Jerala R., Lambeau G., Werz O., Zimmermann R., Petan T. (2023) Lipid droplets control mitogenic lipid mediator production in human cancer cells. Mol. Metab., 76:101791

Dahlke P., Peltner L., Jordan P.M., Werz O. (2023) Differential impact of 5-lipoxygenase-activating protein (FLAP) antagonists on the biosynthesis of leukotrienes and of specialized proresolving mediators (SPM). Front. Pharmacol., 14:1219160

Wollnitzke P., Wagner R., Afsar S.Y., Werner M., Müller C.E., Werz O., van Echten-Deckert G., Menche D. (2023). Total synthesis and biological evaluation of simplified ajudazol derivatives reveal potent 5-lipoxygenase inhibition and considerable apoptotic activity in neuroblastoma cells. Bioorg. Med. Chem. Lett., 94:129464

Schädel P., Wichmann-Costaganna M., Czapka A., Gebert N., Ori A., Werz O. (2023) Short-term caloric restriction and subsequent re-feeding com-promise liver health and associated lipid mediator signaling in aged mice. Nutrients, 15(16):3660

Mikutis S., Lawrinowitz S., Kretzer C., Dunsmore L., Sketeris L., Rodrigues T., Werz O., Bernardes G. J. L. (2023) ACS Chem Biol, 19(1):217-229

Behnke M., Vollrath A., Dahlke P., Páez Larios F., Chi M., Tsarenko E., Jordan P.M., Weber C., Dirauf M., Czaplewska J.A., Beringer-Siemers B., Stumpf S., Kellner C., Kretzer C., Hoeppener S., Nischang I., Sierka M., Eggeling C., Werz O., Schubert U.S. (2023) PEtOxylated polyesteramide nanoparticles for the delivery of anti-inflammatory drugs. Mater Today Chem, 35; 101848

Riedl R., Kühn A., Hupfer Y., Hebecker B., Peltner L.K., Jordan P.M., Werz O., Lorkowski S., Wiegand C., Wallert M. (2023) Characterization of Different Inflammatory Skin Conditions in a Mouse Model of DNCB-induced Atopic Dermatitis. Inflammation, in press
2022
Schubert M., Kluge S., Brunner E., Pace S., Birringer M., Werz O., Lorkowski S. (2022) The α-tocopherol-derived long-chain metabolite α-13'-COOH mediates endotoxin tolerance and modulates the inflammatory response via MAPK and NFκB pathways. Free Radic Biol Med 178:83-96

Jordan P.M., Werz O. (2022) Specialized pro-resolving mediators: Biosynthesis and biological role in bacterial infections. FEBS J., 289(14):4212-4227

Czapka A., Grune C., Schädel P., Bachmann V., Scheuer K., Dirauf M., Weber C., Skaltsounis A., Jandt K.D., Schubert U.S., Fischer D., Werz O. (2022) Drug delivery of 6-bromoindirubin-3’-glycerol-oxime ether employing poly(D,L-lactide-co-glycolide)-based nanoencapsulation techniques with sustainable solvents. J Nanobiotechnology, 20(1):5

Troisi F., Pace S., Jordan P.M., Meyer K.P.L., Bilancia R., Ialenti A., Borelli F., Rossi A., Sautebin L., Serhan C.N., Werz O. (2022) Sex hormone-dependent lipid mediator formation in male and female mice during peritonitis. Front Pharmacol, 12:818544

Kretzer C., Jordan P.M., Bilancia R., Rossi A., Gür T.M., Banoglu E., Schubert U.S., Werz O. (2022) Shifting the biosynthesis of leukotrienes towards specialized pro-resolving mediators by the 5-lipoxygenase-activating protein (FLAP) antagonist BRP-201. J Inflamm Res, 15:911-925

Saviano A., De Vita S., Chini M.G., Marigliano N., Lauro G., Casillo G.M., Raucci F., Iorizzi M., Hofstetter R.K., Fischer K., Koeberle A., Werz O., Maione F., Bifulco G. (2022) In Silico, In Vitro, and In Vivo Analysis of Tanshinone IIA and Cryptotanshinone from Salvia miltiorrhiza as Modulators of Cyclooxygenase-2/mPGES-1/Endothelial Prostaglandin EP3 Pathway. Biomolecules, 12(1):99

Miek L., Jordan P., Guenther K., Beyer T., Kowalak D., Hoerr V., Loeffler B., Tuchscherr L., Serhan C.N., Gerstmeier J., Werz O. (2022) Staphylococcus aureus controls eicosanoid and specialized pro-resolving mediator production via lipoteichoic acid. Immunology, 166(1):47-67

Eckenstaler R., Ripperger A., Hauke M., Petermann M., Hemkemeyer S.A., Schwedhelm E., Ergün S., Frye M., Werz O., Koeberle A., Braun H., Benndorf R.A. (2022) A thromboxane A2 receptor-dependent feedback loop that affects the homeostasis and angiogenic capacity of endothelial cells. Arterioscler Thromb Vasc Biol, 42(4):444-461

Ergül A.G., Gür Maz T., Kretzer C., Olğaç A., Jordan P.M., Çalışkan B., Werz O., Banoglu E. (2022) Novel potent benzimidazole-based microsomal prostaglandin E2 Synthase-1 (mPGES-1) inhibitors derived from BRP-201 that also inhibit leukotriene C4 synthase. Eur J Med Chem, 231:114167

Grosse M., Günther K., Jordan P.M., Roman D., Werz O., Beemelmanns C. (2022) Synthesis of functionalized δ-hydroxy-β-keto esters and evaluation of their anti-inflammatory properties. ChemBioChem, 23(9):e202200073

Knauthe A., Mittag S., Bloch L., Albring K.F., Schmidt M., Werz O., Huber O. (2022) Hyperforin and myrtucommulone derivatives act as natural modulators of Wnt/β-catenin signaling in HCT116 colon cancer cells. Int J Mol Sci, 23(6):2984

Colarusso E., Potenza M., Lauro G., Chini M.G., Sepe V., Zampella A., Fischer K., Hofstetter R.K., Werz O., Bifulco G. (2022) Thiazolidin-4-one-based compounds interfere with the eicosanoid biosynthesis pathways by mPGES-1/sEH/5-LO multi-target inhibition. Eur. J. Med. Chem. Rep., 5; 100046

Napagoda M., Gerstmeier J., Butschek H., Lorenz S., De Soyza S., Qader M., Nagahawatte A., Wijayaratne G.B., Schneider B., Svatoš A., Jayasinghe L., Koeberle A., Werz O. (2022) Plectranthus Zeylanicus: A Rich Source of Secondary Metabolites with Antimicrobial, Disinfectant and Anti-Inflammatory Activities. Pharmaceuticals, 15(4):436

Wang W., Ning Y., Wang Y., Deng G., Pace S., Barth S.A., Menge C., Zhang K., Dai Y., Cai Y., Chen X., Werz O. (2022) Mycobacterium tuberculosis-induced upregulation of the COX-2/ mPGES-1 pathway in human macrophages is abrogated by sulfasalazine. Front Immunol, 13:849583

Zhang K., Jordan P.M., Pace S., Hofstetter R.K., Werner M., Chen X., Werz O. (2022) Modulation of inflammation-related lipid mediator pathways by celastrol during human macrophage polarization. J Inflamm Res, 15:3285-3304

Çapan I., Jordan P.M., Olğaç A., Çalışkan B., Kretzer C., Werz O., Banoglu E. (2022) Discovery and optimization of piperazine urea derivatives as soluble epoxide hydrolase (sEH) inhibitors. ChemMedChem, e202200137

Cerqua I., Neukirch K., Terlizzi M., Granato E., Caiazzo E., Cicala C., Ialenti A., Capasso R., Werz O., Sorrentino R., Seraphin D., Helesbeux J.J., Cirino G., Koeberle A., Roviezzo F., Rossi A. (2022) A vitamin E long-chain metabolite and the inspired drug candidate α-amplexichromanol relieve asthma features in an experimental model of allergen sensitization. Pharmacol Res, 181:106250

Speckmann B., Kleinbölting J., Börner F., Jordan P.M., Werz O., Pelzer S., Tom Dieck H., Wagner T., Schön C. (2022) Synbiotic compositions of Bacillus megaterium and polyunsaturated fatty acid salt enable self-sufficient production of specialized pro-resolving mediators. Nutrients, 14(11):2265

Zahel P., Beekmann U., Eberlein T., Schmitz M., Werz O., Kralisch D. (2022) Bacterial Cellulose – A Nature-Identical Material for Advanced Chronic Wound Care. Pharmaceuticals, 15(6):683

Dunsmore L., Navo C.D., Becher J., Gil de Montes E., Guerreiro A., Hoyt E., Brown L., Zelenay V., Mikutis S., Cooper J., Barbieri I., Lawrinowitz S., Siouve E., Martin E., Ruivo P.R., Rodrigues T., da Cruz F.P., Werz O., Vassiliou G., Ravn P., Jiménez-Osés G., Bernardes G.J.L. (2022) Controlled masking and targeted release of redox-cycling ortho-quinones via a C–C bond-cleaving 1,6-elimination. Nat Chem, 14(7):754-765.

Gazzillo E., Terracciano S., Ruggiero D., Potenza M., Chini M.G., Lauro G., Fischer K., Hofstetter R.K., Giordano A., Werz O., Bruno I., Bifulco G. (2022). Repositioning of quinazolinedione-based compounds on soluble epoxide hydrolase (sEH) through 3D structure-based pharmacophore model-driven investigation. Molecules, 27(12):3866.

Siwczak F., Cseresnyes Z., Abdelwahab M.I., Kehinde H., Aina O., Carlstedt S., Sigmund A., Groger M., Surewaard B.G.J., Werz O., Figge M. T., Tuchscherr L., Löffler B., Mosig A. (2022) Human macrophage polarization determines bacterial persistence of Staphylococcus aureus in a liver-on-chip-based infection model. Biomaterials, 287:121632

Garcia-Moreno M., Jordan P.M., Günther K., Dau T., Fritzsch C., Vermes M., Schoppa A., Ignatius A., Wildemann B., Werz O., Löffler B., Tuchscherr L. (2022) Osteocytes serve as a reservoir for intracellular persisting Staphylococcus aureus due to the lack of defense mechanisms. Front Microbiol, 13:937466.

Wurlitzer J.M., Stanišić A., Ziethe S., Jordan P.M., Günther K., Werz O., Kries H., Gressler M. (2022) Macrophage-targeting oligopeptides from Mortierella alpina. Chem Sci. 15;13(31):9091-9101

Di Micco S., Terracciano S., Pierri M., Cantone V., Liening S., König S., Garscha U., Hofstetter R.K., Koeberle A., Werz O., Bruno I., Bifulco G. (2022) Identification of 2,4-Dinitro-Biphenyl-Based Compounds as MAPEG Inhibitors. ChemMedChem., 17(22):e202200327

Vieider L,. Zoeller E., Romp E., Schoenthaler M., Hernández-Olmos V., Temml V., Hasenoehrl T., Schuster D., Werz O., Garscha U., Matuszczak B. (2022) Synthesis and structure-activity relationships for some novel diflapolin derivatives with benzimidazole subunit. J Enzyme Inhib Med Chem. 37(1):1752-1764.

Bruno F., Krauth V., Nabavi S.M., Temml V., Fratianni F., Spaziano G., Nazzaro F., Roviezzo F., Xiao J., Khan H., Romano M.P., D'Agostino B., Werz O., Filosa R. (2022) Design and synthesis of functionalized 4-aryl-Catechol derivatives as new antiinflammtory agents with in vivo efficacy. Eur J Med Chem. 243:114788.

Turanlı S., Ergül A.G., Jordan P.M., Olğaç A., Çalışkan B., Werz O., Banoglu E. (2022) Quinazoline-4(3H)-one-7-carboxamide Derivatives as Human Soluble Epoxide Hydrolase Inhibitors with Developable 5-Lipoxygenase Activating Protein Inhibition. ACS Omega. 2022 7(41):36354-36365.

Rao Z., Caprioglio D., Gollowitzer A., Kretzer C., Imperio D., Collado J.A., Waltl L., Lackner S., Appendino G., Muñoz E., Temml V., Werz O., Minassi A., Koeberle A. (2022) Rotational constriction of curcuminoids impacts 5-lipoxygenase and mPGES-1 inhibition and evokes a lipid mediator class switch in macrophages. Biochem Pharmacol. 203:115202

Döding A., Hüfner M., Michler F., Iffarth V.K., Bölter A., Bastian A., Symmank J., Andreas N., Schädel P., Thürmer M., Becker K., Wolf M., Jacobs C., Kamradt T., Koeberle A., Werz O., Sigusch B., Schulze-Späte U. (2022) Mediterranean Diet component oleic acid increases protective lipid-mediators and improves trabecular bone in a Porphyromonas-gingivalis-inoculation-model. J Clin Periodontol., 50(3):380-395

Cerqua I., Musella S., Peltner L.K., D'Avino D., Di Sarno V., Granato E., Vestuto V., Di Matteo R., Pace S., Ciaglia T., Bilancia R., Smaldone G., Di Matteo F., Di Micco S., Bifulco G., Pepe G., Basilicata M.G., Rodriquez M., Gomez-Monterrey I.M., Campiglia P., Ostacolo C., Roviezzo F., Werz O., Rossi A., Bertamino A. (2022) Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: In Vitro and In Vivo Anti-Inflammatory Characterization. J Med Chem. 65(21):14456-14480.

Krauth V., Bruno F, Pace S, Jordan PM, Temml V, Preziosa Romano M, Khan H, Schuster D, Rossi A, Filosa R, Werz O. (2022) Highly potent and selective 5-lipoxygenase inhibition by new, simple heteroaryl-substituted catechols for treatment of inflammation. Biochem Pharmacol. 2022 Dec 16:115385

Potenza M., Giordano A., Chini M., Saviano A., Kretzer C., Raucci F., Russo M., Lauro, G., Terracciano S., Bruno I., Iorizzi M., Hofstetter R., Pace S., Maione F., Werz O.*, Bifulco G.* (2022) Identification of 2-aminoacyl-1,3,4-thiadiazoles as prostaglandin E2 and leukotriene biosynthesis inhibitors. ACS Med Chem Lett, 14(1):26-34.
2021
Gilbert N.C., Newcomer M.E., Werz O. (2021) Untangling the web of 5-lipoxygenase-derived products from a molecular and structural perspective: the battle between pro- and anti-inflammatory lipid mediators. Biochem Pharmacol, 193:114759

Werz O. (2020) Cyclooxygenase. Encyclopedia of Molecular Pharmacology, 1-8

Uebbing S., Kreiß M., Scholl F., Häfner A.-K., Sürün D., Garscha U., Werz O., Basavarajappa D., Samuelsson B., Rådmark O., Suess B., Steinhilber D. (2021) Modulation of microRNA processing by 5-lipoxygenase. FASEB J, 35, e21193

Liening S., Fischer J., Jagusch H., Pohnert G., Höcker O., Neusüß C., Werz O., Scriba G., Garscha U. (2021) 12-Oxo-10-glutathionyl-5,8,14-eicosatrienoic acid (TOG10), a novel glutathione-containing eicosanoid generated via the 12-lipoxygenase pathway in human platelets. Prostaglandins Other Lipid Mediat., 152, 106480

Grune C., Thamm J., Werz O., Fischer D. (2021) Cyrene^TM as an alternative sustainable solvent for the preparation of poly(lactic-co-glycolic acid) nanoparticles. J Pharm Sci, 110, 959-964.

Grune C., Zens C., Czapka A., Scheuer K., Thamm J., Hoeppener S., Jandt K.D., Werz O., Neugebauer U., Fischer D. (2021) Sustainable preparation of anti-inflammatory atorvastatin PLGA nanoparticles. Int J Pharm 599:120404

Deinhardt-Emmer S., Böttcher S., Häring C., Giebeler L., Henke A., Zell R., Jungwirth J., Jordan P., Werz O., Hornung F., Brandt C., Marquet M., Mosig A., Pletz M., Schacke M., Roedel J., Heller R., Nietzsche S., Loeffler B., Ehrhardt C. (2021) SARS-CoV-2 causes severe epithelial inflammation and barrier dysfunction. J Virol, 95(10):e00110-21.

Schädel P., Troisi F., Czapka A., Gebert N., Pace S., Ori A., Werz O. (2021) Aging drives organ-specific alterations of the inflammatory microenvironment guided by immunomodulatory mediators in mice. FASEB J, 35(5):e21558

Pace S., Zhang K., Jordan P.M., Bilancia R., Wang W., Börner F., Hofstetter K., Potenza M., Kretzer C., Gerstmeier G., Fischer D., Lorkowski S., Gilbert N.C., Newcomer M.E., Rossi A., Chen X., Werz O. (2021) Anti-inflammatory celastrol promotes a switch from leukotriene biosynthesis to formation of specialized pro-resolving lipid mediators. Pharmacol Res, 167:105556

Kim M., Kim G., Kang M., Ko D., Nam Y., Moon C.S., Kang M.H., Shin J.-S., Werz O., Lee K.T., Lee J.Y. (2021) Discovery of N-Amido-Phenylsulfonamide Derivatives as Novel Microsomal Prostaglandin E2 Synthase-1 (mPGES-1) Inhibitors. Bioorg Med Chem Lett, 41:127992

Kühne M., Kretzer C., Lindemann H., Godmann M., Heinze T., Werz O., Heinzel T. (2021) Biocompatible valproic acid-coupled nanoparticles attenuate lipopolysaccharide-induced inflammation. Int J Pharm, 601:120567

Gürses T., Olgaç A., Garscha U., Maz T.G., Bal N.B., Uludağ O., Çalışkan B., Schubert U.S., Werz O., Banoglu E. (2021) Simple heteroaryl modifications in the 4,5-diarylisoxazol-3-carboxylic acid scaffold favorably modulates the activity as dual mPGES-1/5-LO inhibitors with in vivo efficacy. Bioorg Chem, 112:104861

Di Micco S., Terracciano S., Ruggiero D., Potenza M., Vaccaro M., Fischer K., Werz O., Bruno I., Bifulco G. (2021) Identification of 2-(thiophen-2-yl) acetic acid-based lead compound for mPGES-1 Inhibition. Front Chem, 9:676631

Anh T.T.V., Mostafa A., Rao Z., Pace S., Schwaiger S., Kretzer C., Temml V., Giesel C., Jordan P.M., Bilancia R., Weinigel C., Rummler C., Waltenberger B., Hung T., Rossi A., Stuppner H., Werz O.*, Koeberle A.* (2021) From Vietnamese plants to a biflavonoid that relieves inflammation by triggering the lipid mediator class switch to resolution. Acta Pharmaceutica Sin, 11(6):1629-1647

Willems S., Gellrich L., Chaikuad A., Kluge S., Werz O., Heering J., Knapp S., Lorkowski S., Schubert-Zsilavecz M., Merk D. (2021) Endogenous vitamin E metabolites mediate allosteric PPARγ activation with unprecedented co-regulatory interactions. Cell Chem Biol, 28(10):1489-1500

Jagusch H., Werner M., Koenis D., Dalli J., Werz O., Pohnert G. (2021) 14,17,18-Trihydroxy-Eicosatetraenoic Acid: A Novel Pro-Resolving Lipid Mediator from Marine Microalgae. ACS Pharmacol Transl Sci, 4(3):1188-1194

Zhang K., Pace S., Jordan P.M., Peltner L.K., Weber A., Fischer D., Hofstetter R.K., Chen X., Werz O. (2021) Beneficial Modulation of Lipid Mediator Biosynthesis in Innate Immune Cells by Antirheumatic Tripterygium wilfordii Glycosides. Biomolecules, 11(5):746

Friedrich L., Cingolani G., Ko Y.-H., Iaselli M., Miciaccia M., Perrone M.G., Neukirch K., Bobinger V., Merk D., Hofstetter R.K., Werz O., Koeberle A., Scilimati A., Schneider G. (2021) Learning from nature: From a marine natural product to synthetic cyclooxygenase-1 inhibitors by automated de novo design. Adv. Sci., 8(16):e2100832

Jordan P.M., Andreas N., Groth M., Wegner P., Weber F., Jäger U., Küchler C., Werz O., Serfling E., Kamradt T., Dudeck A., Drube S. (2021) ATP/IL-33-triggered hyperactivation of mast cells results in an amplified production of pro-inflammatory cytokines and eicosanoids. Immunology 164(3):541-554.

Ning Y., Cai Y., Dai Y., Li F., Mo S., Werz O., Chen X. (2021) Mitochondrial fusion mediated by mitofusin 1 regulates macrophage mycobactericidal activity by enhancing autophagy. Infect Immun, 89(11):e0030621

Börner F., Werner M., Ertelt J., Meins J., Abdel-Tawab M., Werz O. (2021) Analysis of boswellic acid contents and related pharmacological activities of frankincense-based remedies that modulate inflammation. Pharmaceuticals, 14(7):660

Vollrath A., Kretzer C., Beringer-Siemers B., Shkodra B., Czaplewska J.A., Bandelli D., Stumpf S., Hoeppener S., Weber C., Werz O., Schubert US (2021) Effect of Crystallinity on the Properties of Polycaprolactone Nanoparticles Containing the Dual FLAP/mPEGS-1 Inhibitor BRP-187. Polymers, 13(15):2557

Potenza M., Sciarretta M., Festa C., Chini M.G., De Marino S., Hofstetter R.K., D’Auria M.V., Werz O., Bifulco G. (2021) Structure-based screening for the discovery of 1,2,4-oxadiazoles as promising hits for the development of new anti-inflammatory agents interfering with eicosanoid biosynthesis pathways. Eur J Med Chem, 224:113693

Neukirch K., Alsabil K., Dinh C-P., Bilancia R, Raasch M., Ville A., Cerqua I., Viault G., Bréard D., Pace S., Temml V., Brunner E., Jordan P., Marques M., Loeser K., Gollowitzer A., Permann S., Gerstmeier, Jana; J., Lorkowski S., Stuppner H., Garscha U., Rodrigues T., Bernardes G., Schuster D., Seraphin D., Richomme P., Rossi A., Mosig A., Roviezzo F., Werz O.*, Helesbeux J.-J.*, Koeberle A.* (2021) Exploration of long-chain vitamin E metabolites for the discovery of a highly potent, orally effective and metabolically stable 5-LOX inhibitor that limits inflammation. J Med Chem, 64:11496-11526.

Hoff J., Karl B., Gerstmeier J., Beekmann U., Schmölz L., Börner F., Kralisch D., Bauer M., Werz O., Fischer D., Lorkowski S., Press A.T. (2021) Controlled release of the α-tocopherol-derived metabolite α-13’-carboxychromanol from bacterial nanocellulose wound cover improves wound healing. Nanomaterials, 11(8):1939

Fischer J., Gresnigt M.S., Werz O., Hube B., Garscha U. (2021) Candida albicans-induced leukotriene biosynthesis in neutrophils is restricted to the hyphal morphology. FASEB J, 35:e21820.

Penkert H., Bertrand A., Tiwari V., Breimann S., Müller S.A., Jordan P.M., Gerl M.J., Klose C., Cantuti-Castelvetri L., Bosch-Queralt M., Levental I., Lichtenthaler S.F., Werz O., Simons M. (2021) Proteomic and lipidomic profiling of demyelinating lesions identifies fatty acids as modulators in lesion recovery. Cell Rep., 37:109898

Wolfram T., Weidenbach L.M., Adolf J., Schwarz M., Schädel P., Gollowitzer A., Werz O., Koeberle A., Kipp A.P., Koeberle S.C. (2021) The trace element selenium is important for redox signaling in phorbol ester-differentiated THP-1 macrophages. Int J Mol Sci, 22(20):11060

Grune C., Kretzer C., Zergiebel S., Kattner S., Thamm J., Hoeppener S., Werz O., Fischer D. (2021) Encapsulation of the anti-inflammatory dual FLAP/sEH inhibitor diflapolin improves the efficiency in human whole blood. J Pharm Sci, 111(6):1843-1850

Jordan P.M., van Goethem E., Müller A.M., Hemmer K., Gavioli V., Baillif V., Burmeister Y., Krömmelbein N., Dubourdeau M., Seilheimer B., Werz O. (2021) The Natural Combination Medicine Traumeel (Tr14) Improves Resolution of Inflammation by Promoting the Biosynthesis of Specialized Pro-Resolving Mediators. Pharmaceuticals, 4(11):1123.

Kretzer C., Jordan P.M., Meyer K.P.L., Hoff D., Werner M., Hofstetter R.K., Koeberle A., Peralta A.C., Viault G., Seraphin D., Richomme R., Helesbeux J.-J., Stuppner H., Temml V., Schuster D., Werz O. (2022). Natural chalcones elicit formation of specialized pro-resolving mediators and related 15-lipoxygenase products in human macrophages. Biochem Pharmacol, 195:114825

Kretzer C., Shkodra B., Klemm P., Jordan P.M., Schröder D., Cinar G., Vollrath A., Schubert S., Nischang I., Hoeppener S., Stumpf S., Banoglu E., Gladigau F., Bilancia R., Rossi A., Eggeling C., Neugebauer U., Schubert U.S., Werz O. (2021) Ethoxy acetalated dextran-based nanocarriers accomplish efficient inhibition of leukotriene formation by a novel FLAP antagonist in human leukocytes and blood. Cell Mol Life Sci, 79(1):40

Andreas N., Müller S., Templin N., Jordan P.M., Schuhwerk H., Müller M., Gerstmeier J., Miek L., Andreas S., Werz O., Kamradt T. (2021) Incidence and severity of G6PI-induced arthritis are not increased in genetically distinct mouse strains upon aging. Arthritis Res Ther. 23(1):222.

Müller A.K., Albrecht F., Rohrer C., Koeberle A., Werz O., Schlörmann W., Glei M., Lorkowski S., Wallert M. (2021) Olive Oil Extracts and Oleic Acid Attenuate the Lps-Induced Inflammatory Response in Murine RAW264.7 Macrophages but Induce the Release of Prostaglandin E2. Nutrients, 13(12):4437
2020
Wallert M., Kluge S., Schubert M., Koeberle A., Werz O., Birringer M., Lorkowski S. (2020) Diversity of chromanol and chromenol structures and functions: an emerging class of anti-inflammatory and anti-carcinogenic agents. Front Pharmacol., 11:362.

Pace S. Werz O. (2020) Impact of androgens on inflammation-related lipid mediator biosynthesis in innate immune cells. Front Immunol, 11:1356.

Serhan C.N., Gupta S.K., Perretti M., Godson C., Brennan E., Li Y., Soehnlein O., Shimizu T., Werz O., Chiurchiù V., Azzi A., Dubourdeau M., Gupta S.S., Schopohl P., Hoch M., Gjorgevikj D., Khan F.M., Brauer D., Tripathi A., Cesnulevicius K., Lescheid D., Schultz M., Särndahl E., Repsilber D., Kruse R., Sala A., Haeggström J.Z., Levy B.D., Filep J.G., Wolkenhauer O. (2020) The Atlas of Inflammation Resolution (AIR). Mol Aspects Med, 74:100894

Romp E., Arakandy V., Fischer J., Wolz C., Siegmund A., Löffler B., Tuchscherr L., Werz O., Garscha U. (2020) Exotoxins from Staphylococcus aureus activate 5-lipoxygenase and induce leukotriene biosynthesis. Cell Mol Life Sci, 77, 3841-3858

Koeberle S.C., Gollowitzer A., Laoukili J., Kranenburg O., Werz O., Koeberle A., Kipp AP. (2020) Distinct and overlapping functions of glutathione peroxidases 1 and 2 in limiting NF-κB-driven inflammation through redox-active mechanisms. Redox Biol, 28, 101388

Werner M., Pace S., Czapka A., Jordan P., Gerstmeier J., Koeberle A., Werz O. (2020) Communication between human macrophages and epithelial cancer cell lines dictates lipid mediator biosynthesis. Cell Mol Life Sci, 77, 4365-4378

Wang W., Deng G., Zhang G., Yu Z., Yang F., Chen J., Cai Y., Werz O., Chen X. (2020). Genetic polymorphism rs8193036 of IL17A is associated with increased susceptibility to pulmonary tuberculosis in Chinese Han population. Cytokine, 127:154956.

Traeger A., Voelker S., Shkodra-Pula B., Kretzer C., Schubert S., Gottschaldt M., Schubert U.S. Ulrich, Werz O. (2020) Improved bioactivity of the natural product 5-lipoxygenase inhibitor hyperforin by encapsulation into polymeric nanoparticles. Mol Pharm, 17, 810-816.

Lauro G, Terracciano S, Cantone V, Ruggiero D, Fischer K, Pace S, Werz O, Bruno I, Bifulco G. (2020) A Combinatorial Virtual Screening Approach Driving the Synthesis of 2,4-Thiazolidinedione-Based Molecules as New Dual mPGES-1/5-LO Inhibitors. ChemMedChem, 5, 481-489.

Rao Z., Jordan P.M., Wang Y., Menche D., Pace S., Gerstmeier J., Werz O. (2020) Differential role of vacuolar (H+)-ATPase in the expression and activity of cyclooxygenase-2 in human monocytes. Biochem Pharmacol., 175, 113858.

Olgac A., Carotti, A., Kretzer C., Zergiebel S., Seeling A., Garscha U., Werz O., Macchiarulo A., Banoglu E. (2020) Discovery of novel 5-lipoxygenase-activating protein (FLAP) inhibitors by exploiting a multistep virtual screening protocol. J Chem Inf Model, 60, 1737-1748

Beekmann U., Schmölz L., Lorkowski S., Werz O., Thamm J., Fischer D., Kralisch D. (2020 Process control and scale-up of modified bacterial cellulose production for tailor-made anti-inflammatory drug delivery systems. Carbohydr Polym, 236:116062

Chini M.G., Giordano A., Potenza M., Terracciano S., Fisher K., Vaccaro M.C., Colarusso E., Bruno I., Riccio R., Koeberle A., Werz O., Bifulco G. (2020) Targeting mPGES-1 by a combinatorial approach: identification of the aminobenzothiazole scaffold to suppress PGE2 levels. ACS Med. Chem Lett, 11, 783-789

Gilbert N.C., Gerstmeier J., Schexnaydre E.E., Börner F., Garscha U., Neau D.B., Werz O.*, Newcomer M.E.* (2020) Structural and mechanistic insights into 5-lipoxygenase inhibition by natural products. Nat Chem Biol, 16, 783-790

Gebert N., Cheng C.W., Kirkpatrick J.M., Di Fraia D., Yun J., Schädel P., Pace S., Garside G.B., Werz O., Rudolph K.L., Jasper H., Yilmaz Ö., Ori A. (2020) Region-specific proteome changes of the intestinal epithelium during aging and dietary restriction, Cell Rep, 31, 107565

Wang W., Cai Y., Deng G., Yang Q., Tang P., Wu M., Yu Z., Yang F., Chen J., Werz O.*, Chen X.* (2020) Allelic specific regulation of xCT expression increases susceptibility to tuberculosis by modulating miRNA–mRNA interactions. mSphere, 5, e00263-20

Hanke T., Cheung SY., Kilu W., Heering J., Ni X., Planz V., Schierle S., Faudone G., Friedrich M., Wanior M., Werz O., Windbergs M., Proschak E., Schubert-Zsilavecz M., Chaikuad A., Knapp S., Merk D. (2020) A selective modulator of peroxisome proliferator pro-liferator-activated receptor γ with unprecedented binding mode. J Med Chem, 63, 4555-4561

Napagoda M., Gerstmeier J., Butschek H., De Soyza S., Pace S., Lorenz S., Qader M., Witharana S., Nagahawatte A., Wijayaratne G., Svatoš A., Jayasinghe L., Koeberle A., Werz O. (2020) On the anti-inflammatory and antimicrobial potential of selected ethnomedicinal plants from Sri Lanka. Molecules, 25, 1894

Shkodra-Pula B., Kretzer C., Jordan P.M., Klemm P., Koeberle A., Pretzel D., Banoglu E., Lorkowski S., Wallert M., Höppener S., Stumpf S., Vollrath A., Schubert S., Werz O.*, Schubert U.S.* (2020) Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity. J Nanobiotechnology, 18, 73.

Stürner K. H., Werz O., Koeberle A., Otto M., Pless O., Leypoldt F., Paul F., Heesen C. (2020) Lipid mediator profiles predict response to therapy with an oral frankincense extract in relapsing-remitting multiple sclerosis. Sci Rep, 10, 8776

Cerqua I., Terlizzi M., Bilancia R., Riemma M.A., Citi V., Martelli A., Pace S., Spaziano G., D’Agostino B., Werz O., Ialenti A., Sorrentino R., Cirino G., Rossi A., Roviezzo F. (2020) 5α-dihydrotestosterone abrogates sex bias in asthma like features in the mouse. Pharmacol Res, 158, 104905

Dinh C.P., Ville A, Neukirch K., Viault G., Temml V., Koeberle A., Werz O., Schuster D., Stuppner H., Richomme P., Helesbeux J.-J., Séraphin D. (2020) Structure-based design, semi-synthesis and anti-inflammatory activity of tocotrienolic amides as 5-lipoxygenase inhibitors. Eur J Med Chem, 202, 112518.

Karl B., Alkhatib Y., Beekmann U., Bellmann T., Blume G., Steiniger F., Thamm J., Werz O., Kralisch D., Fischer D. (2020) Development and Characterization of Bacterial Nanocellulose Loaded with Boswellia Serrata Extract Containing Nanoemulsions as Natural Dressing for Skin Diseases. Int J Pharm., 587, 119635

Czapka A., König S., Pergola C., Grune C., Vougogiannopoulou K., Skaltsounis A.L., Fischer D., Werz O. (2020) The indirubin derivative 6-bromoindirubin-3’-glycerol-oxime ether (6BIGOE) potently modulates inflammatory cytokine and prostaglandin release from human monocytes through GSK-3 interference. Biochem Pharmacol, 180, 114170

Espada L., Dakhovnik A., Chaudhari P., Martirosyan A., Miek L., Poliezhaieva T., Schaub Y., Nair A., Döring N., Rahnis N., Werz O., Koeberle A., Kirkpatrick J., Ori A., Ermolaeva M. (2020) Loss of metabolic plasticity underlies metformin toxicity in aged Caenorhabditis elegans. Nat Metab, 2, 1316-1331

Jordan P.M., Gerstmeier J., Pace S., Bilancia R., Rao Z., Börner F., Miek L., Gutiérrez-Gutiérrez O., Arakandy V., Rossi A., Ialenti A., González-Estévez C., Löffler B., Tuchscherr L., Serhan C.N., Werz O. (2020) Staphylococcus aureus-derived α-hemolysin evokes generation of specialized pro-resolving mediators promoting inflammation resolution. Cell Rep, 33, 108247

Mayr F., Möller G., Garscha U., Fischer J., Rodríguez Castaño P., Inderbinen S.G., Temml V., Waltenberger B., Schwaiger S., Hartmann R.W., Gege C., Martens S., Odermatt A., Pandey A.V., Werz O., Adamski J., Stuppner H., Schuster D. (2020) Finding New Molecular Targets of Familiar Natural Products Using In Silico Target Prediction. Int. J. Mol. Sci., 21, 7102

Behnke M., Vollrath A., Klepsch L., Beringer-Siemers B., Stumpf S., Czaplewska J.A., Hoeppener S., Werz O., Schubert U.S. (2020) Optimized Encapsulation of the FLAP/PGES-1 Inhibitor BRP-187 in PVA-Stabilized PLGA Nanoparticles Using Microfluidics. Polymers, 12, 2751

Beekmann U, Zahel P, Karl B, Schmölz L, Börner F, Gerstmeier J, Werz O, Lorkowski S, Wiegand C, Fischer D, Kralisch D. (2020) Modified Bacterial Cellulose Dressings to Treat Inflammatory Wounds. Nanomaterials, 10(12):2508
2019
Shekfeh S., Çalışkan B., Fischer K., Yalçın T., Garscha U., Werz O., Banoglu E. (2018) A multi-step virtual screening protocol for identification of novel non-acidic microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors. ChemMedChem, 14, 273-281.

Schexnaydre E.E., Gerstmeier J., Garscha U., Jordan P.J., Werz O., Newcomer M.E. (2019) A 5-Lipoxygenase-Specific Sequence Motif Impedes Enzyme Activity and Confers Dependence on a Partner Protein. Biochim Biophys Acta Mol Cell Biol Lipids, 1864, 543-551

Fettel J., Kühn B., Guillen N.A., Sürün D., Peters M., Bauer R., Angioni C., Geisslinger G., Schnütgen F., Meyer zu Heringdorf D., Werz O., Meybohm P., Zacharowski K., Steinhilber D., Roos J., Maier T. J. (2018) Sphingosine-1-phosphate induces potent anti-inflammatory effects in vitro and in vivo by sphingosine-1-phosphate receptor 4-mediated suppression of 5-lipoxygenase activity. FASEB J., 33, 1711-1726

Rossi A., Roviezzo F., Sorrentino R., Riemma M.A., Cerqua I., Bilancia R., Spaziano G., Troisi F., Pace S., Pinto A., D’Agostino B., Werz O., Cirino G., (2019) Leukotriene-mediated sex dimorphism in murine asthma-like features during allergen sensitization. Pharmacol. Res., 139,182-190

König S., Romp E., Krauth V., Rühl M., Dörfer M., Liening S., Hofmann B., Häfner A.-K., Steinhilber D., Karas M., Garscha U., Hoffmeister D., Werz O. (2019) Melleolides from honey mushroom inhibit 5-lipoxygenase via Cys159. Cell Chem Biol, 26, 60-70

König S., Pace S., Pein H., Heinekamp T., Kramer J., Romp E., Straßburger M., Troisi F., Proschak A., Dworschak J., Scherlach K., Rossi A., Sautebin L., Haeggström J.Z., Hertweck C., Brakhage A.A., Gerstmeier G., Proschak E., Werz O. (2018) Gliotoxin from Aspergillus fumigatus abrogates leukotriene B4 formation through inhibition of leukotriene A4 hydrolase. Cell Chem Biol, 26, 524-534

Werner M., Jordan P. M., Romp E., Czapka A., Rao Z., Kretzer C., Koeberle A., Garscha U., Pace S., Claesson H.-E., Serhan C. N., Werz O., Gerstmeier J (2018) Targeting biosynthetic networks of the pro-inflammatory and pro-resolving lipid metabolome. FASEB J. 33, 6140-6153

Gerstmeier J., Kretzer C., Di Micco S., Miek L., Butschek H., Cantone V., Bilancia R., Rizza R., Troisi F., Cardullo N., Tringali C., Ialenti A., Rossi A., Bifulco G., Werz O.*, Pace S. (2019). Novel benzoxanthene lignans that favorably modulate lipid mediator biosynthesis: a promising pharmacological strategy for anti-inflammatory therapy. Biochem Pharmacol, 165, 263-274.

Wallert M., Bauer J., Kluge S., Schmölz L., Chen Y.-C., Ziegler M., Searle A.K., Maxonese A., Schubert M., Thürmer M., Pein H., Koeberle A., Werz O., Birringer M., Peter K., Lorkowski S. (2019). The vitamin E derivative garcinoic acid from Garcinia kola nut seeds attenuates the inflammatory response. Redox Biol, 24, 101166

Dörfer M., Heine D., König S., Gore S., Werz O., Hertweck C., Gressler M., Hoffmeister D. (2019) Melleolides impact fungal translation via elongation factor 2. Org Biomol Chem 17, 4906-4916

Nausch B., Pace S., Pein H., Koeberle A., Rossi A., Kuenstle G., Werz O. (2019) The standardized herbal combination BNO 2103 contained in Canephron N alleviates inflammatory pain in experimental cystitis and prostatitis. Phytomedicine, 60:152987

Jagusch H., Werner M., Okuno T., Yokomizo T., Werz O.*, Pohnert G.* (2019) An Alternative Pathway to Leukotriene B4 Enantiomers Involving a 1,8-diol-Forming Reaction of an Algal Oxylipin. Org Lett, 21, 4667-4670

Freund R.R.A., Gobrecht P., Rao Z., Gerstmeier G., Schlosser R., Görls H., Werz O., Fischer D., Arndt H.-D. (2019) Stereoselective total synthesis of parthenolides indicates target selectivity for tubulin carboxypeptidase activity. Chem Sci 10, 7358-7364

Rao Z., Pace S., Jordan P.M., Bilancia R., Troisi F., Börner F., Andreas N., Kamradt T., Menche D., Rossi A., Serhan C.N., Gerstmeier J., Werz O. (2019) Vacuolar (H+)-ATPase critically regulates specialized pro-resolving mediator pathways in human M2-like monocyte-derived macrophages and resolution of inflammation. J Immunol, 203, 1031-1043

Gerstmeier J., Seegers J., Witt F., Waltenberger B., Temml V., Rollinger J.M., Stuppner H., Koeberle A., Schuster D., Werz O. (2019) Ginkgolic acid is a multi-target inhibitor of key enzymes in pro-inflammatory lipid mediator biosynthesis. Front Pharmacol 10, 797

Lee H.-H., Moon Y.H., Shin J.-S., Lee J.-H., Kim T.-W., Jang C., Park C., Lee J., Kim Y., Kim Y., Werz O., Park B.Y., Lee J.Y., Lee K.-T. (2019) A novel mPGES-1 inhibitor alleviates inflammatory responses by downregulating PGE₂ in experimental models. Prostaglandins Other Lipid Mediat, 144, 106347

Bartel K., Pein H., Popper B., Schmitt S., Janaki-Raman S., Schulze A., Lengauer F., Koeberle A., Werz O., Zischka H, Müller R, Vollmar AM, von Schwarzenberg K (2019) Connecting lysosomes and mitochondria – a novel role for lipid metabolism in cancer cell death. Cell Commun Signal 17, 87

Klapper M., Paschold A., Zhang S., Weigel C., Dahse H.M., Götze S., Pace S., König S., Rao Z., Reimer L., Werz O., Stallforth P. (2019) Bioactivity and Mode of Action of Bacterial Tetramic Acids. ACS Chem Biol, 14, 1693-1697.

Liening S., Romp E., Werz O., Scriba G.K.E., Garscha U. (2019) Liquid chromatography-coupled mass spectrometry analysis of glutathione conjugates of oxygenated polyunsaturated fatty acids. Prostaglandins Other Lipid Mediat, 144, 106350.

Cirri E., De Decker S., Bilcke G., Werner M., Osuna-Cruz C. M., De Veylder L., Vandepoele K., Werz O., Vyverman W., Pohnert G. (2019) Associated bacteria affect sexual reproduction by altering gene expression and metabolic processes in a biofilm inhabiting diatom. Front Microbiol 10, 1790.

Aluwi M. F. F. M., Rullah K., Koeberle A., Werz O., Razak N.S.A., Wei L. S., Abas F., Ismail N.H., Jantan I., Wai L.K. (2019) Design and synthesis of a novel mPGES-1 lead inhibitor guided by 3D-QSAR CoMFA. J Mol Struct, 1196, 844-850

Sester A., Winand L., Pace S., Hiller W., Werz O.*, Nett M.* (2019) Myxochelin- and Pseudochelin-Derived Lipoxygenase Inhibitors from a Genetically Engineered Myxococcus xanthus strain. J Nat Prod 82, 2544-2549

Boccellino M., Donniacuo M., Bruno F., Rinaldi B., Quagliuolo L., Ambruosi M., Pace S., De Rosa M., Olgaç A., Banoglu E., Alessio N., Massa A., Kahn H., Werz O., Fiorentino A., Filosa R. (2019) Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors. Eur J Med Chem, 180, 637-647

Jagusch H., Werner M., Werz O.*, Pohnert G.* (2019) 15‐Hydroperoxy‐PGE₂ – A Novel Intermediate in Mammalian and Algal Prostaglandin Biosynthesis Angew Chem Int Ed Engl, 58, 17641-17645

Hiesinger K., Schott A., Kramer J., Blöcher R., Witt F., Wittmann S., Steinhilber D., Pogoryelov D., Gerstmeier J., Werz O., Proschak E. (2019) Design of dual inhibitors of soluble epoxide hydrolase and LTA₄ hydrolase. ACS Med Chem Lett., 11, 298-302.

Romp E., Arakandy V., Fischer J., Wolz C., Siegmund A., Löffler B., Tuchscherr L., Werz O., Garscha U. (2019) Exotoxins from Staphylococcus aureus activate 5-lipoxygenase and induce leukotriene biosynthesis. Cell Mol Life Sci, in press

Zhang K., Wang X., Tu J., Rong H., Werz O., and Chen X. (2019) The interplay between depression and tuberculosis. J Leuk Biol, 127, 154956
2018
Glatzel D.K., Koeberle A., Pein H., Loeser K., Stark A., Keksel N., Werz O., Mueller R., Bischoff I., Fuerst R. (2018) Acetyl-CoA carboxylase 1 regulates endothelial cell migration by shifting the phospholipid composition. J Lipid Res., 59, 298-311

Stürner K.H., Stellmann J.-P., Dörr J., Paul F., Friede T., Schammler S., Reinhardt S., Siemonsen S., Weissflog G., Faizy T., Werz O., Fleischer S., Vaas L. A. I., Herrmann F., Pless O., Martin R., Heesen C. (2018) A Standardized Frankincense Extract Reduces Disease Activity in Relapsing-Remitting Multiple Sclerosis (The SABA phase IIa trial). J Neurol Neurosurg Psychiatry, 89, 330-338

Dawczynski C., Dittrich M., Neumann T., Goetze K., Welzel A., Oelzner P., Völker S., Schaible A.M., Troisi F., Thomas L., Pace S., Koeberle A., Werz O., Schlattmann P., Lorkowski S., Jahreis G (2018) Docosahexaenoic acid in the treatment of rheumatoid arthritis: A double-blind, placebo-controlled, randomized cross-over study with microalgae vs. sunflower oil. Clin Nutr, 37, 494-504

Roos J., Peters M., Maucher I.V., Kühn B., Fettel J., Hellmuth N., Brat C., Sommer B., Urbschat A., Piesche M., Vogel A., Proschak E., Blöcher R., Buscato E., Häfner A.K., Matrone C., Werz O., Heidler J., Wittig I., Angioni C., Geisslinger G., Parnham M.J., Zacharowski K., Steinhilber D., Maier T.J. (2018) Drug-mediated intracellular donation of nitric oxide potently inhibits 5-lipoxygenase: a possible key to future anti-leukotriene therapy. Antioxid Redox Signal, 28, 1265-1285

Werz O., Gerstmeier J., Libreros S., De la Rosa X., Werner M., Norris PC., Chiang N., Serhan CN (2018) Human macrophages differentially produce specific resolvin or leukotriene signals that depend on bacterial pathogenicity. Nat Commun, 9, 59

Stoiber K., Nagło O., Pernpeintner C., Zhang S., Koeberle A., Ulrich M., Werz O., Mueller R., Zahler S., Lohmüller T., Feldmann J., Braig S. (2018) Targeting de novo lipogenesis as a novel approach in anti-cancer therapy. Br J Cancer, 118, 43-51

Di Micco S., Terracciano S., Cantone V., Fischer K., Koeberle A., Foglia A., Riccio R., Werz O., Bruno I., Bifulco G. (2018) Discovery of new potent molecular entities able to inhibit mPGES-1. Eur J Med Chem, 143, 1419-1427

Seibel J., Wonnemann M., Werz O., Lehner M.D. (2018) A tiered approach to investigate the mechanism of anti-inflammatory activity of an herbal medicinal product containing a fixed combination of thyme herb and primula root extracts. Clin Phytoscience, 4, 4

Gür Z.T., Çalışkan B., Garscha U., Olgaç A., Schubert U.S., Gerstmeier J., Werz O., Banoglu E. (2018) Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7. Eur J Med Chem., 150, 876-899

Rettener J., Werner M., Meyer N., Werz O., Pohnert G. (2018) Survey of the C20 and C22 oxylipin family in marine diatoms. Tetrahedron lett., 9, 828-831

Koeberle A., Henkel A., Verhoff M., Tausch L., König S., Fischer D., Kather N., Seitz S., Paul M., Jauch J., Werz O. (2018) Triterpene acids from frankincense and semi-synthetic derivatives that inhibit 5-lipoxygenase and cathepsin G. Molecules, 23, pii: E506

Loeser K., Seemann S., König S., Lehnhardt I., Abdel-Tawab M., Koeberle A., Werz O., Lupp A. (2018) Protective effect of Casperome®, an orally bioavailable frankincense extract, on lipopolysaccharide-induced systemic inflammation in mice. Front. Pharmacol., 9, 387

Napagoda M., Gerstmeier J., Butschek H., Lorenz S., Kanatiwela D., De Soyza S., Qader M., Nagahawatte A., Wijayaratne G. B., Svatoš A., Jayasinghe L., Koeberle A., Werz O. (2018) Lipophilic extracts of Leucas zeylanica, a multi-purpose medicinal plant in the tropics, inhibit key enzymes involved in inflammation and gout. J Ethnopharmacol, 224, 474-481

Bruno F., Errico S., Pace S., Nawrozkij M.B., Guida F., Maisto R., Olgaç A., D’Amico M., Maione S., Banoglu E., De Rosa M., Werz O., Fiorentino A., Filosa R. (2018) Structural Insight into the Optimization of Ethyl 5-Hydroxybenzo[g]indol-3-carboxylates and their Bioisosteric Analogues as 5-LO/m-PGES-1 Dual Inhibitors Able to Suppress Inflammation. Eur J Med Chem, 155, 946-960

Guo H., Benndorf R., König S., Leichnitz D., Weigel C., Peschel G., Berthel P., Kaiser M., Steinbeck C., Werz O., Poulsen M.T., Beemelmanns C. (2018) Expanding the Rubterolone Family – Intrinsic Reactivity and Directed Diversification of PKS-derived Pyrans. Chem Eur J, 4, 11319-11324

Rodrigues T., Werner M., Roth J., da Cruz E. H. G, Marques M. C., Akkapeddi P., Lobo S.A., Koeberle A., Corzana F., da Silva Junior E. N., Werz O., Bernardes G. J. L. (2018) Machine intelligence decrypts b-lapachone as an allosteric 5-lipoxygenase inhibitor. Chem Sci, 9, 6899-6903

Cheung S.-Y., Werner M., Esposito L., Troisi F., Cantone V., Liening S., König S., Gerstmeier J., Koeberle A., Bilancia R., Rizza R., Rossi A., Roviezzo F., Temml V., Schuster D., Stuppner H., Schubert-Zsilavecz M., Werz O.*, Thomas Hanke T.*, Pace S. (2018) Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation. Eur J Med Chem, 156, 815-830

Pein H., Ville A., Pace S., Temml V., Garscha U., Raasch M., Alsabil K., Viault G., Dinh C-P., Guilet D., Troisi F., Neukirch K., König S., Bilancia R., Waltenberger B., Stuppner H., Wallert M., Lorkowski S., Weinigel C., Rummler S., Birringer M., Roviezzo F., Sautebin L., Helesbeux J.-J., Séraphin D., Mosig A., Schuster D., Rossi A., Richomme P., Werz O.*, Koeberle A.* (2018) Endogenous metabolites of vitamin E limit inflammation by targeting 5 lipoxygenase.Nat Commun, 9, 3834

Meyer N., Rettner J., Werner M., Werz O., Pohnert G. (2018) Algal oxylipins mediate the resistance of diatoms against algicidal bacteria. Mar Drugs, 16, pii: E486.

Vieider L., Romp E., Temml V., Kretzer C., Schoenthaler M., Taha A., Fischer J., Hernández-Olmos V., Sturm S., Schuster D., Werz O., Garscha U., Matuszczak B. (2018) Synthesis, biological evaluation and structure-activity relationships of diflapolin analogs as dual sEH/FLAP inhibitors. ACS Med Chem Lett., 10, 62-66

Lauro G., Cantone V., Potenza M., Fischer K., Koeberle A., Werz O., Riccio R., Bifulco G. (2018) Discovery of 3-hydroxy-3-pyrrolin-2-one-based mPGES-1 inhibitors using a multi-step virtual screening protocol. MedChemComm, 9, 2028-2036.

Koeberle A., Werz O. (2018) Natural products as inhibitors of prostaglandin E₂ and pro-inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis. Biotechnol Adv, 36, 1709-1723.
2017
Grisoni F., Reker D., Schneider P., Friedrich L., Consonni V., Todeschini R., Koeberle A., Werz O., Schneider G. (2016) Matrix-based molecular descriptors for prospective virtual compound screening. Mol Inform, 36(1-2). doi: 10.1002/minf.201600091.

Lauro G., Manfra M., Pedatella S., Fischer K., Cantone V., Terracciano S., Bertamino A., Ostacolo C., Gomez-Monterrey I., De Nisco M., Riccio R., Novellino E., Werz O., Campiglia P., Bifulco G. (2017) Identification of novel microsomal prostaglandin E2 synthase-1 (mPGES-1) lead inhibitors from Fragment Virtual Screening. Eur J Med Chem 125, 278-287

Peduto A., Scuotto M., Krauth V., Roviezzo F., Rossi A., Temml V., Esposito V., Stuppner H., Schuster D., D’Agostino B., Schiraldi C., de Rosa M., Werz O.*, Filosa R.* (2017) Optimization of Benzoquinone and Hydroquinone Derivatives as Potent Inhibitors of Human 5-Lipoxygenase. Eur J Med Chem 127, 715-726

Bartel K., Winzi M., Ulrich M., Koeberle A., Menche D., Werz O., Müller R., Guck J., Vollmar A., von Schwarzenberg K. (2017) V-ATPase inhibition increases cancer cell stiffness and blocks membrane related Ras signaling - a new option for HCC therapy. Oncotarget, 8, 9476-9487

Schieferdecker S, König S, Pace S, Werz O*, Nett M* (2017) Myxochelin-Inspired 5-Lipoxygenase Inhibitors - Synthesis and Biological Evaluation. ChemMedChem 12, 23-27

Pergola C., Schubert K., Pace S., Ziereisen J., Nikels F., Scherer O., Hüttel S., Zahler S., Vollmar A., Weinigel C., Rummler S., Müller R., Raasch M., Mosig A., Koeberle A., Werz O. (2017) Modulation of actin dynamics as potential macrophage subtype-targeting anti-tumour strategy. Sci Rep, 7, 41434

Temml V., Garscha U., Romp E., Schubert G., Gerstmeier J., Kutil Z., Matuszczak M., Waltenberger B., Stuppner H., Werz O.*, Schuster D.* (2017) Discovery of the first dual inhibitor of the 5-lipoxygenase-activating protein and soluble epoxide hydrolase using pharmacophore-based virtual screening. Sci Rep 7, 42751

Allegrone G., Pollastro F., Magagnini G., Taglialatela-Scafati O., Seegers J., Koeberle A., Werz O.*, Appendino G*. (2017) The Bibenzyl Canniprene Inhibits the Production of Pro-Inflammatory Eicosanoids and Selectively Accumulates in Some Cannabis sativa Strains. J Nat Prod, 80, 731-734

Thomas L., Rao Z., Gerstmeier J., Raasch M., Weinigel C., Rummler S., Menche D., Müller R., Pergola C., Mosig A., Werz O. (2017) Selective upregulation of TNFα expression in classically-activated human monocyte-derived macrophages (M1) through pharmacological interference with V-ATPase. Biochem Pharmacol, 130, 71-82

Svouraki A., Garscha U., Kouloura E., Pace S., Pergola C., Krauth V., Rossi A., Sautebin L., Halabalaki M., Werz O.*, Gaboriaud-Kolar N., Skaltsounis A.L.* (2017) Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-type Isoprenylated Acetophenones, J Nat Prod, 80, 699-706

Siemoneit, U., Tausch, L., Poeckel, D., Paul M., Northoff H., Koeberle A., Jauch, J., and Werz, O. (2017) Defined structure-activity relationships of boswellic acids determine modulation of Ca²⁺ mobilization and aggregation of human platelets by Boswellia serrata extracts. Planta Med., 83, 1020-1027

Wiechmann K., Müller H., König S., Wielsch N., Svatoš A., Jauch J., Werz O. (2017) Mitochondrial chaperonin HSP60 is the apoptosis-related target for myrtucommulone. Cell Chem Biol, 24, 614-623.

Pace S., Rossi A.*, Krauth V., Dehm F., Troisi F., Bilancia R., Weinigel C., Rummler S., Werz O.*, Sautebin L. (2017) Sex differences in prostaglandin biosynthesis in neutrophils during acute inflammation. Sci Rep, 7, 3759

Pace S., Pergola C., Dehm F., Rossi A., Gerstmeier J., Troisi F., Pein H., Schaible A.M., Weinigel C., Rummler S., Northoff H., Laufer S., Maier T.J., Rådmark O., Samuelsson B., Koeberle A., Sautebin L., Werz O. (2017) Androgen-mediated sex bias impairs efficiency of leukotriene biosynthesis inhibitors in males. J Clin Invest, 127, 3167-3176

Pein H., Koeberle S.C., Voelkel M., Schneider F., Rossi A., Thürmer M., Loeser K., Sautebin L., Morrison H., Werz O., Koeberle A. (2017) Vitamin A regulates Akt signaling through the phospholipid fatty acid composition. FASEB J, 31, 4566-4577

Garscha U., Romp E., Pace S., Rossi A., Temml V., Schuster D., König S., Gerstmeier J., Liening S., Werner M., Atze H., Wittmann S., Weinigel C., Rummler S., Scriba G., Sautebin S., Werz O. (2017) Pharmacological profile and efficiency in vivo of diflapolin, the first dual inhibitor of 5-lipoxygenase-activating protein and soluble epoxide hydrolase. Sci Rep, 7, 9398

Schmölz L., Wallert M., Rozzino N., Cignarella A., Galli F, Glei M., Werz O., Koeberle A., Birringer M., Lorkowski S. (2017) Structure-function relationship studies in vitro reveal distinct and specific effects of long-chain metabolites of vitamin E. Mol Nutr Food Res, 61, doi: 10.1002/mnfr.201700562

Lopatriello A., Previtera R., Pace S., Werner M., Rubino L., Werz O., Taglialatela-Scafati O., Forino M. (2017) NMR-based identification of the major bioactive molecules from an Italian cultivar of Lycium barbarum. Phytochemistry, 144, 52-57

Werz O., Gerstmeier J. Garscha U. (2017) Novel leukotriene biosynthesis inhibitors (2012-2016) as anti-inflammatory agents. Expert Opin Ther Pat, 5, 1-14

Pace S., Sautebin L., Werz O. (2017) Sex-biased eicosanoid biology: impact for sex differences in inflammation and consequences for pharmacotherapy. Biochem Pharmacol, 145, 1-11
2016
Di Micco S., Spatafora C., Cardullo N., Riccio R., Fischer K., Pergola C., Koeberle A., Werz O., Chalal M., Vervandier-Fasseur D., Tringali C., Bifulco G. (2016) 2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors. Bioorg Med Chem 24, 820-826

Essig S., Schmalzbauer B., Bretzke S., Scherer O., Koeberle A., Werz O., Müller R., Menche D. (2016) Predictive Bioinformatic Assignment of Methyl-Bearing Stereocenters: Total Synthesis and an Additional Molecular Target of Ajudazol B. J Org Chem 81,1333-57

Gerstmeier J., Newcomer M.E., Dennhardt S., Romp E., Fischer J., Werz O., Garscha U. (2016) 5-Lipoxygenase-Activating Protein rescues activity of 5-lipoxygenase mutations that delay nuclear membrane association and disrupt product formation. FASEB J 30, 1892-1900

Lauro G., Tortorella P., Bertamino A., Ostacolo C., Koeberle A., Fischer K., Bruno I., Terracciano S., Gomez-Monterrey I.M., Tauro M., Loiodice F., Novellino E., Riccio R., Werz O., Campiglia P., Bifulco G. (2016) Structure based design of mPGES-1 inhibitors using a Virtual Fragment growing optimization scheme. ChemMedChem 11, 612-619

Rossi A., Pace S., Tedesco F., Pagano E., Guerra G., Troisi F., Werner M., Roviezzo F., Zjawiony J.K., Werz O., Izzo A.A., Capasso R. (2016) The hallucinogenic diterpene salvinorin A inhibits leukotriene synthesis in experimental models of inflammation. Pharmacol Res 106, 64-71

Waltenberger B., Garscha U., Temml V., Liers J., Werz O., Schuster D., Stuppner H. (2016) Discovery of Potent Soluble Epoxide Hydrolase (sEH) Inhibitors by Pharmacophore-Based Virtual Screening. J Chem Inf Model 56, 747-762

Banoglu E., Çelikoğlu E., Völker S., Olgaç A, Gerstmeier J., Garscha U., Çalışkan B., Schubert U.S., Carotti A., Macchiarulo A., Werz O. (2016) 4,5-Diarylisoxazol-3-carboxylic acids: a new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP). Eur J Med Chem 113,1-10

Forino M., Pace S., Chianese G., Santagostini L., Werner M., Weinigel C., Rummler S., Fico G., Werz O.*, Taglialatela-Scafati O*. (2016) Humudifucol and Bioactive Prenylated Polyphenols from Hop (Humulus lupulus cv. Cascade). J Nat Prod, 79, 590-597

Chindo B.A., Schröder H., Koeberle A., Werz O., Becker A. (2016) Analgesic potential of standardized methanol stem bark extract of Ficus plathyphylla in mice: Mechanisms of action. J Ethnopharmacol. 184:101-106

Schaible A.M., Filosa R., Krauth V., Temml V., Pace S., Garscha U., Liening S., Weinigel C., Rummler S., Schieferdecker S., Nett M., Peduto A., Collarile S., Scuotto M., Roviezzo F., Spaziano G., de Rosa M., Stuppner H., Schuster D., D’Agostino B., Werz O. (2016) The 5-lipoxygenase inhibitor RF-22c potently suppresses leukotriene biosynthesis in cellulo and blocks bronchoconstriction and inflammation in vivo. Biochem. Pharmacol. 112, 60-71

Alsabil K., Suor-Cherer S., Koeberle A., Viault G., Lavaud A., Temml V., Waltenberger B., Schuster D., Litaudon M., Lorkowski S., de Vaumas R., Helesbeux J.J., Guilet D., Stuppner H., Werz O., Seraphin D., Richomme P. (2016) Semisynthetic and Natural Garcinoic Acid Isoforms as New mPGES-1 Inhibitors. Planta Med., 82, 1110-1116

Levent S., Gerstmeier J., Olgaç A., Nikels F., Garscha U., Carotti A., Macchiarulo A., Werz O., Banoglu E., Çalışkan B. (2016) Synthesis and biological evaluation of C(5)-substituted derivatives of leukotriene biosynthesis inhibitor BRP-7. Eur J Med Chem. 122, 510-519

Maione F., Cantone V., Pace S., Chini M.G., Bisio A., Romussi G., Pieretti S., Werz O., Koeberle A., Mascolo N., Bifulco G. (2016) In vivo and in vitro biological evaluation of the anti-inflammatory and analgesic response of carnosol and carnosic acid and in silico analysis of their target interactions. Br J Pharmacol, 174, 1497-1508

Aligiannis N., Halabalaki M., Chaita E., Kouloura E., Argyropoulou A., Benaki D., Kalpoutzakis E., Angelis A., Stathopoulou K., Antoniou S., Sani M., Krauth V., Werz O., Schütz B., Schäfer H., Spraul M., Mikros E., Skaltsounis L.A. (2016) Heterocovariance Based Metabolomics as a Powerful Tool Accelerating Bioactive Natural Product Identification. ChemistrySelect, 1, 2531–2535

Liening S., Scriba G.K.E., Rummler S., Weinigel C., Kleinschmidt T.K., Haeggström J.Z., Werz O., Garscha U. (2016) Development of smart cell-free and cell-based assay systems for investigation of leukotriene C4 synthase activity and evaluation of inhibitors. Biochim Biophys Acta 1861, 1605-1613

Garscha U., Voelker S., Pace S., Gerstmeier J., Emini B., Liening S., Rossi A., Weinigel C., Rummler S., Schubert U.S., Scriba G.K.E., Çelikoğlu E., Çalışkan B., Banoglu E., Sautebin L., Werz O. (2016) BRP-187: a potent inhibitor of leukotriene biosynthesis that acts through impeding the dynamic 5-lipoxygenase / 5-lipoxygenase-activating protein (FLAP) complex assembly. Biochem Pharmacol 119, 17-26

Röhrl J., Werz O., Ammendola A., Künstle G. (2016) Vitex agnus-castus dry extract BNO 1095 (Agnucaston®) inhibits uterine hyper-contractions and inflammation in experimental models for primary dysmenorrhea. Clin Phytosci, 2, 20. DOI 10.1186/s40816-016-0034-3

Park E.B., Kim K.J., Jeong H.R., Lee J.K., Kim H.J., Lee H.H., Lim J.W., Shin J.-S., Koeberle A., Werz O., Lee K.T., Lee J.Y. (2016) Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents. Bioorg Med Chem Lett 26, 5193-5197

Roos J., Grösch S., Werz O., Schröder P., Ziegler S., Fulda S., Paulus P., Urbschat A., Kühn B., Maucher I., Fettel J., Vorup-Jensen T., Piesche M., Steinhilber D., Parnham M.J., Maier T.J. (2016) Regulation of tumorigenic Wnt signaling by cyclooxygenase-2, 5-lipoxygenase and their pharmacological inhibitors: a basis for novel drugs targeting cancer cells? Pharmacol & Ther 157, 43-64

Koeberle A., Laufer S., Werz O. (2016) Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions. J Med Chem 59, 5970-5986
2015
Roos J., Grösch S., Werz O., Schröder P., Ziegler S., Fulda S., Paulus P., Urbschat A., Kühn B., Maucher I., Fettel J., Vorup-Jensen T., Piesche M., Steinhilber D., Parnham M.J., Maier T.J. (2015) Regulation of tumorigenic Wnt signaling by cyclooxygenase-2, 5-lipoxygenase and their pharmacological inhibitors: a basis for novel drugs targeting cancer cells? Pharmacol & Ther, 157, 43-64

Kim M., Lee S., Park E.B., Kim K.J., Lee H.H., Shin J.-S., Fischer K., Koeberle A., Werz O.*, Lee K.-T.,* Lee J.Y.* (2015) Hit-to-lead optimization of phenylsulfonyl hydrazides for a potent suppressor of PGE2 production: Synthesis, biological activity, and molecular docking study. Bioorg Med Chem Lett, 26, 5193-5197

Iranshahi M., Chini M., Masullo M., Sahebkar A., Javidnia A., Chitsazian Yazdi M., Pergola C., Koeberle A., Werz O., Pizza C., Terracciano S., Piacente S., Bifulco G. (2015) Can small chemical modifications of natural pan-inhibitors modulate the biological selectivity? The case of curcumin prenylated derivatives acting as HDAC or mPGES-1 inhibitors. J Nat Prod, 108, 466-475

Peduto A., Krauth V., Collarile S., Dehm F., Ambruosi M., Belardo C., Guida F., Massa A., Esposito V., Maione S., De Rosa M., Werz O., Filosa R. (2015) Exploring the role of chloro and methyl substitutions in 2-phenylthiomethylbenzoindole derivatives for 5-LOX enzyme. Eur J Med Chem, 108, 466-475

Werz O., and Radmark, O. (2015) 5-Lipoxygenase. Progress in Inflammation Research: Lipoxygenases in Inflammation, 978-3-319-27764-6

Seidel J., Pergola C., Werz O., Kryshen K., Wosikowski K., Lehner M.D., Haunschild J. (2015) Bronchipret® Syrup containing thyme and ivy extracts suppresses bronchoalveolar inflammation and goblet cell hyperplasia in experimental bronchoalveolitis. Phytomedicine, 22, 1172-1177

Wolfram S., Wielsch N., Hupfer Y., Mönch B., Lu-Walther H.-W., Heintzmann R., Werz O., Svatoš A., Pohnert G., (2015) A metabolic probe-enabled strategy reveals uptake and protein targets of polyunsaturated aldehydes in the diatom Phaeodactylum tricornutum. PLoS ONE, 10:e0140927

Wiechmann K., Müller H., Fischer D., Jauch J., Werz O. (2015) The acylphloroglucinols hyperforin and myrtucommulone A cause mitochondrial dysfunctions in leukemic cells by direct interference with mitochondria. Apoptosis, 20, 1508-17

Korp J., König S., Schieferdecker S., Dahse H.M., König G.M., Werz O., Nett M. (2015) Harnessing Enzymatic Promiscuity in Myxochelin Biosynthesis for the Production of 5-Lipoxygenase Inhibitors. ChemBioChem, 16, 2445-2450

Henkel A., Tausch L., Pillong M., Jauch J., Karas M., Schneider G., Werz O. (2015) Boswellic acids target the human immune system-modulating antimicrobial peptide LL-37. Pharmacol Res, 102, 53-60

Gerstmeier J., Weinigel C., Rummler S., Rådmark O., Werz O., Garscha U. (2015) Time-resolved in situ assembly of the leukotriene-synthetic 5-LO / FLAP complex in blood leukocytes. FASEB J, 30, 276-285

Häfner A.-K., Gerstmeier J., Hörnig M., George S., Ball A.-K., Schröder M., Garscha U., Werz O., Steinhilber D. (2015) Characterization of the interaction of human 5-lipoxygenase with its activating protein FLAP. Biochim Biophys Acta, 185, 1465-72

Ciffolilli S., Wallert M., Bartolini D., Krauth V., Werz O., Piroddi M., Sebastiani B., Torquato P., Lorkowski S., Birringer M., Galli F. (2015) Human serum determination and in vitro anti-inflammatory activity of the vitamin E metabolite α-(13'-hydroxy)-6-hydroxychroman. Free Radic Biol Med, 89, 952-962

De Lucia D., Lucio O. M., Musio B., Bender A., Listing M., Dennhardt S., Koeberle A., Garscha U., Rizzo R., Manfredini S., Werz O., Ley S.V. (2015) Design, Synthesis and Evaluation of Semi-Synthetic Triazole-containing Caffeic Acid Analogues as 5-Lipoxygenase Inhibitors. Eur J Med Chem, 101, 573-83

Braig S., Schmidt B.U.S, Ferkaljuk K., Händel C., Möhn T., Werz O. , Müller R., Zahler S., Koeberle A., Käs J. A., Vollmar A.M. (2015) Pharmacological targeting of membrane rigidity: Implications on cancer cell migration and invasion. New J Phys, 17, 083007
Koeberle A. and Werz O. (2015) Perspective of microsomal prostaglandin E2 synthase-1 as drug target in inflammation-related disorders. Biochem Pharmacol, 98, 1-15

Noha S., Fischer K., Koeberle A., Garscha U., Werz O., Schuster D. (2015) Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol Bioorg Med Chem, 23, 4839-45

Wiechmann K., Müller H., Huch V., Hartmann D., Werz O., Jauch J. (2015) Synthesis and Biological Evaluation of Novel Myrtucommulones and Structural Analogues that Target mPGES-1 and 5-Lipoxygenase. Eur J Med Chem, 101, 133-49

Merk D., Zettl M., Steinhilber D., Werz O., Schubert-Zsilavecz M. (2015) Pirinixic acids - flexible fatty acid mimetics with various biological activities. Future Med Chem, 7, 1598-616

Wallert M., Schmölz L., Koeberle A., Krauth V., Glei M., Galli F., Werz O., Birringer M., Lorkowski S. (2015) The α-tocopherol long-chain metabolite α-13'-COOH affects the inflammatory response of lipopolysaccharide-activated murine RAW264.7 macrophages. Mol Nutr Food Res, 59, 1524-34

Filosa R., Peduto A., Schaible A.M., Krauth V., Weinigel C., Barz D., Petronzi C., Bruno F., Roviezzo F., Spaziano G., D'Agostino B., De Rosa M., Werz O. (2015) Novel series of benzoquinones with high potency against 5-lipoxygenase in human polymorphonuclear leukocytes. Eur J Med Chem, 94, 132-9

Scherer O., Maeß M., Lindner S., Garscha U., Weinigel C., Rummler S., Werz O., Lorkowski S. (2015) A procedure for efficient non-viral siRNA transfection of primary human monocytes using nucleofection. J Immunol Methods, 4722, 118-24

Schieferdecker S., König S., Koeberle A., Dahse H.-M., Werz O. and Nett M. (2015) Myxochelins target human 5-lipoxygenase. J Nat Prod, 78, 335-8

Koeberle A., Pergola C., Shindou H., Koeberle S.C., Shimizu T., Laufer S.A. and Werz O. (2015) Role of p38 mitogen-activated protein kinase in linking stearoyl-CoA desaturase-1 activity with ER homeostasis. FASEB J, 29, 2439-49

Pergola C., Schaible A.M., Nikels F., Dodt G., Northoff H. and Werz O. (2015) Progesterone rapidly down-regulates the biosynthesis of 5-lipoxygenase products in human primary monocytes. Pharmacol Res, 94, 42-50

Grandjenette C., Schnekenburger M., Morceau F., Mack F., Wiechmann K., Werz O., Dicato M. and Diederich M. (2014) Dual Induction of Mitochondrial Apoptosis and Senescence in Chronic Myelogenous Leukemia by Myrtucommulone A. Anticancer Agents Med Chem, 15, 363-73

Terracciano S., Lauro G., Strocchia M., Fischer K., Werz O., Riccio R., Bruno I. and Bifulco G. (2014) Structural insights for the optimization of dihydropyrimidin-2(1H)-one based mPGES-1 inhibitors. ACS Med Chem Lett, 6, 187-91

Winekenstädde D., Angelis A., Waltenberger B., Schwaiger S., Tchoumtchoua J., König S., Werz O., Aligiannis N., Skaltsounis A.L. and Stuppner H. (2014) Phytochemical Profile of the Aerial Parts of Sedum sediforme and Anti-inflammatory Activity of Myricitrin. Nat Prod Comun, 10, 83-88

Flesch D., Ness J., Lamers C., Dehm F., Popella S., Steri R., Ogorek I., Hieke M., Dannhardt G., Werz O., Weggen S. and Schubert-Zsilavecz M. (2014) SAR-studies of γ-secretase modulators with PPARγ-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease. Bioorg Med Chem Lett, 24, 841-6
2014
Chini M.G., Cantone V., Ferroni C., Dambruoso P., Varchi G., Pepe A, Fischer K., Pergola C., Werz O., Bruno I., Riccio R., Bifulco G. (2014) Elucidating new structural features of the triazole scaffold for the development of mPGES-1 inhibitor. MedChemComm, 6, 75-79

Rådmark O., Werz O., Steinhilber D. and Samuelsson B. (2014) 5-Lipoxygenase, a key enzyme for leukotriene biosynthesis in health and disease. Biochim Biophys Acta, in press

Werz O., Radmark O. and Steinhilber D. (2014) Recent advances on 5-lipoxygenase biochemistry. eLS: Citable Reviews in the Life Sciences, in press

Reker D., Perna A. M., Rodrigues T., Schneider P., Reutlinger M., Mönch B., Koeberle A., Lamers C., Gabler M., Steinmetz H., Müller R., Schubert-Zsilavecz M., Werz O. and Schneider, G. (2014) Revealing the macromolecular targets of complex natural products. Nat Chem, 6, 1072-8

Bollmann F., Art J., Henke J., Schrick K., Besche V., Bros M., Li H., Siuda D., Handler N., Bauer F., Erker T., Behnke F., Mönch B., Härdle L., Hoffmann M., Chen C.Y., Förstermann U., Dirsch V., Werz O., Kleinert H., Pautz A. (2014) Resveratrol post-transcriptionally regulates pro-inflammatory gene expression via regulation of KSRP RNA binding activity. Nucl Acid Res, 42, 12555-69

Schieferdecker S., König S., Weigel C., Dahse H.M., Werz O. and Nett M. (2014) Structure and Biosynthetic Assembly of Gulmirecins, Macrolide Antibiotics from the Predatory Bacterium Pyxidicoccus fallax. Chem Eur J, 20, 15933-40

Scherer O., Steinmetz H., Kaether C., Weinigel C., Barz D., Kleinert H., Menche D., Müller R., Pergola C. and Werz O. (2014) Targeting V-ATPase in primary human monocytes by archazolid potently represses the classical secretion of cytokines due to accumulation at the endoplasmic reticulum. Biochem Pharmacol, 91, 490-500

Koeberle A. and Werz O. (2014) Multi-target approach for natural products in inflammation. Drug Discov Today, 19, 1871-1882.

Hanke T., Lamers C., Carrasco Gomez R., Schneider G., Werz O. and Schubert-Zsilavecz M. (2014) Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition. Bioorg Med Chem, 24, 3757-63

Bohnert M., Scherer O., Wiechmann K., König S., Dahse H.-M., Hoffmeister D. and Werz O. (2014) Melleolides induce rapid cell death in human primary monocytes and cancer cells. Bioorg Med Chem, 22, 3856-61

Koeberle A., Muñoz E., Appendino G.B., Minassi A., Pace S., Rossi A., Weinigel C., Barz D., Sautebin L., Caprioglio D., Collado J.A. and Werz O. (2014) SAR Studies on Curcumin's Pro-inflammatory Targets: Discovery of Prenylated Pyrazolocurcuminoids as Potent and Selective Novel Inhibitors of 5-Lipoxygenase. J Med Chem, 57, 5638-48

Rossi A., Pergola C., Pace S., Rådmark O., Werz O. and Sautebin L. (2014) In vivo sex differences in leukotriene biosynthesis in zymosan-induced peritonitis. Pharmacol Res, 87, 1-7

Gerstmeier J., Weinigel C., Barz D., Werz O. and Garscha U. (2014) An experimental cell-based model for studying the cell biology and molecular pharmacology of 5-lipoxygenase-activating protein in leukotriene biosynthesis. Biochim Biophys Act, 1840, 2961-9
Verhoff M., Seitz S., Paul M., Noha S., Jauch J., Schuster D. and Werz O. (2014) Tetra- and Pentacyclic Triterpene Acids from the Ancient Anti-inflammatory Remedy Frankincense as Inhibitors of Microsomal Prostaglandin E2 Synthase-1. J Nat Prod, 77, 1445-51

Richter P., Schubert G., Schaible A.M., Cavas L., Werz O.* and Pohnert G.* (2014) Caulerpenyne and related bis-enol esters are novel-type inhibitors of human 5-lipoxygenase. Chem Med Chem, 9, 1655-9 * shared corresponding authorship

Werz O., Seegers J., Schaible A.M., Weinigel C., Barz D., Koeberle A., Allegrone G., Pollastro F., Zampieri L., Grassie G. and Appendino G. (2014) Cannflavins from hemp sprouts, a novel cannabinoid-free hemp food product, target microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. PharmaNutrition, 2, 53-60

Lauro G., Strocchia M., Terracciano S., Bruno I., Fischer K., Pergola C., Werz O., Riccio R. and Bifulco G. (2014) Exploration of the dihydropyrimidine scaffold for the development of new potential anti-inflammatory agents blocking prostaglandin E2 synthase-1 enzyme (mPGES-1). Eur J Med Chem, 80, 407-15

Vougogiannopoulou K., Lemus C., Halabalaki M., Pergola C., Werz O., Smith A.B., Michel S., Skaltsounis L., Deguin B. (2014) One-step Semisynthesis of Oleacein and its Determination as a 5-Lipoxygenase Inhibitor. J Nat Product, 77, 441-5

Pergola C., Gerstmeier J., Mönch B., Çalışkan B., Luderer S., Weinigel C., Barz D., Maczewsky J., Pace S., Rossi A., Sautebin L., Banoglu E. and Werz O. (2014) The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP) Br J Pharmacol, 171, 3051-64

Kubisch R., von Gamm M., Braig S., Ullrich A., Burkhart J.L., Colling L., Hermann J., Scherer O., Müller R., Werz O., Kazmaier U. and Vollmar A.M. (2014) Simplified Pretubulysin Derivatives and Their Biological Effects on Cancer Cells. J Nat Prod, 77, 536-42

Peduto A., Bruno F., Dehm F., Krauth V., De Caprariis P., De Rosa M., Weinigel C., Barz D., Massa A., Werz O. and Filosa R. (2014) Further Studies on Ethyl 5-hydroxy-indole-3-carboxylate scaffold: Design, Synthesis and Evaluation of 2-phenylthiomethyl-Indole Derivatives as Efficient Inhibitors of Human 5-Lipoxygenase. Eur J Med Chem, 81, 492-98

Pergola C.,Gaboriaud-Kolar N., Jestädt N., König S., Kritsanida M., Schaible A.M., Li H., Garscha U., Weinigel C., Barz D., Albring K.F., Huber O., Skaltsounis A.L. and Werz O. (2014) The Indirubin Core Structure of Glycogen Synthase Kinase-3 Inhibitors as Novel Chemotype for Intervention with 5-Lipoxygenase. J Med Chem, 57, 3715-23

Scior T., Verhoff M., Gutierrez-Aztatzi I., Ammon HPT, Laufer S. and Werz O. (2014) Interference of Boswellic Acids with the Ligand Binding Domain of the Glucocorticoid Receptor. J Chem Inf Model, 54, 978-86

Schaible A.M., Filosa R., Temml V., Krauth V., Matteis M., Peduto A., Bruno A.F., Luderer S., Roviezzo F., Di Mola A., de Rosa M., D'Agostino B., Weinigel C., Barz D., Koeberle A., Pergola C., Schuster D. and Werz O. (2014) Elucidation of the molecular mechanism and the efficiency in vivo of a novel 1,4-benzoquinone that inhibits 5-lipoxygenase. Br J Pharmacol, 171, 2399-412

Merk D., Gabler M., Gomez R.C., Flesch D., Hanke T., Kaiser A.,Lamers C., Werz O., Schneider G. and Schubert-Zsilavecz M. (2014) Anthranilic acid derivatives as partial farnesoid X receptor agonists. Bioorg Med Chem, 15, 2447-60

Blažević T., Schaible A.M., Weinhäupl K., Schachner D., Nikels F., Weinigel C., Barz D., Atanasov A.G., Pergola C., Werz O., Dirsch V.M. and Heiss E.H. (2014) Indirubin-3'-monoxime exerts a dual mode of inhibition towards leukotriene-mediated vascular smooth muscle cell migration. Cardiovascular Res, 101, 522-32

Sardella, R., Levent, S., Ianni, F., Çalişkan, B., Gerstmeier, J., Pergola, C., Werz, O., Banoglu, E. and Natalini, B. (2013) Chromatographic separation and biological evaluation of benzimidazole derivative enantiomers as inhibitors of leukotriene biosynthesis. J Pharm Biomed Anal, 89C, 88-92
2013
Napagoda M., Gerstmeier J., Koeberle A, Wesely S., Popella S.D., Lorenz S., Scheubert K., Boecker S, Svatoš A and Werz O. (2013) Munronia pinnata (Wall.) Theob.: Unveiling phytochemistry and dual inhibition of 5-lipoxygenase and microsomal prostaglandin E2 synthase (mPGES)-1. J Ethnopharmacol, 151, 882-90

Napagoda M., Gerstmeier J., Wesely S., Popella S.D., Lorenz S., Scheubert K., Svatoš A and Werz O. (2013) Inhibition of 5-lipoxygenase as anti-inflammatory mode of action of Plectranthus zeylanicus Benth and chemical characterization of ingredients by a mass spectrometric approach. J Ethnopharmacol, 151, 800-09

Hanke T., Dehm F., Liening S., Popella S.D., Maczewsky J., Pillong M., Kunze J., Weinigel C., Barz D., Kaiser A., Wurglics M., Lämmerhofer M., Schneider G., Sautebin L., Schubert-Zsilavecz M. and Werz O. (2013) Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo. J Med Chem, 56, 9031-44

Blažević T., Schwaiberger A.V., Schreiner C.E., Schachner D., Schaible A.M., Grojer C.S., Atanasov G.A., Werz O., Dirsch V.M. and Heiss E.H. (2013) 12/15-Lipoxygenase contributes to Platelet-Derived Growth Factor-Induced Activation of Signal Transducer and Activator of Transcription 3*. J Biol Chem, 288, 35592-603

Krämer, A., Mentrup, T., Kleizen, B., Rivera-Milla, E., Reichenbach, D., Enzensperger, C., Nohl, R., Täuscher, E., Görls, H., Ploubidou, A., Englert, C., Werz, O., Arndt, H.D. and Kaether, C. (2013) Discovery of small molecules for intercepting Notch signaling and the early secretory pathway. Nat Chem Biol, 9, 731-8

Oettl, S., Gerstmeier, J., Khan, S., Wiechmann, K., Bauer, J., Atanasov, A., Malainer, C., Awad, E., Uhrin, P., Heiss, E.H., Waltenbergera, B., Remias, D., Breuss, J., Boustie, J., Dirsch, D.M., Stuppner, H., Werz, O.* and Rollinger, J.M.* (2013) Imbricaric acid and perlatolic acid: Multi-targeting anti-Inflammatory depsides from Cetrelia monachorum. PLOS one, 8, e76929 (* shared corresponding authorship)

Garcia-Alonso, V., Lopez-Vicario, C., Titos, E., Moran, E., Gonzalez-Periz, A., Rius, B., Parrizas, M., Werz, O., Arroyo, V. and Claria, J. (2013) Coordinate functional regulation between microsomal prostaglandin E synthase-1 and PPARγ in the conversion of white-to-brown adipocytes. J Biol Chem, 288, 28230-42

Abromeit, H., Werz, O. and Scriba, G. K.E. (2013) Separation of 5-Lipoxygenase Metabolites using Cyclodextrin-based Microemulsion Electrokinetic Chromatography and Head Column Field Amplified Sample Stacking. Chromatographia, 76, 1187-1192

Filosa, R., Peduto, A., Aparoy, P., Schaible, A.M., Luderer, S., Petronzi, C., Massa, A., de Rosa, M., Reddanna, P. and Werz, O. (2013) Discovery and biological evaluation of novel 1,4-benzoquinone and related resorcinol derivatives that inhibit 5-lipoxygenase. Eur J Med Chem, 67C, 269-279

Schaible, A.M., Koeberle, A., Northoff, H., Lawrenz, B., Weinigel, C., Barz, D., Werz, O. and Pergola, C. (2013) High capacity for leukotriene biosynthesis in peripheral blood during pregnancy. Prostaglandins Leukot Essent Fatty Acids, 89, 245-55

Wagner, M., Werz, O. and Steinhilber, D. (2013) Upregulation of the 5-lipoxygenase pathway in human monocytes by growth and differentiation factors. Pharmazie, 68, 578-83.

Schaible, A.M., Traber, H., Temml, V., Noha, S.M., Filosa, R., Peduto, A., Weinigel, C., Barz, D., Schuster, D. and Werz, O. (2013) Potent inhibition of human 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 by the anti-carcinogenic and anti-inflammatory agent embelin. Biochemical Pharmacol, 86, 476-86

Koeberle, A., Shindou, H., Koeberle, S.C., Laufer, S.A., Shimizu, T. and Werz, O. (2013) Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding. Proc Nat Acad Sci USA, 110, 2546-51
2012
Meins, J., Rossi, A., Sautebin, L., Wiechmann, K., Werz, O., Skarke, C., Barrett, J.S., Schubert-Zsilavecz, M. and Abdel-Tawab, M. (2012) Myrtucommulone from Myrtus communis: metabolism, permeability, and systemic exposure in rats. Planta Med, 78, 1932-8

Gerbeth, K., Hüsch, J., Fricker, G., Werz, O., Schubert-Zsilavecz, M. and Abdel-Tawab, M. (2012) In vitro metabolism and brain availability of six major boswellic acids from Boswellia serrata gum resins. Fitoterapia, 84C, 99-106

Bauer, J., Waltenberger, B., Noha, S.M., Schuster, D., Rollinger, J.M., Boustie, J., Stuppner, H. and Werz, O. (2012) Discovery of depsides and depsidones from lichen as novel, potent inhibitors of microsomal prostaglandin E2 synthase-1 using pharmacophore models. Chem Med Chem, 7, 2077-81

Elkady, M., Niess, R., Schaible, A.M., Bauer. J., Luderer, S., Ambrosi, G., Werz, O. and Laufer, SA. (2012) Modified Acidic Nonsteroidal Anti-Inflammatory Drugs as Dual Inhibitors of mPGES-1 and 5-LOX. J Med Chem, 55, 8958-62

Abromeit, H., Schaible, A.M., Werz, O. and Scriba, G.K.E. (2012) Chemometrics-guided development of a cyclodextrin-modified micellar electrokinetic chromatography method with head-column field amplified sample stacking for the analysis of 5-lipoxygenase metabolites. J Chromatogr A, 1267, 217-23

Babiuch, K., Gottschaldt, M., Werz, O. and Schubert, S.U. (2012) Particulate Transepithelial Drug Carriers: Barriers and Materials. RSC Adv, 2, 10427-10465

De Simone, R., Bruno, I., Riccio, R., Stadler, K., Bauer, J., Schaible, A.M., Laufer, S. and Werz, O. (2012) Identification of new γ-hydroxybutenolides that preferentially inhibit the activity of mPGES-1. Bioorg Med Chem, 20, 5012-6

Verhoff, M., Seitz, S., Northoff, H., Jauch, J., Schaible, A.M. and Werz, O. (2012) A novel C(28)-hydroxylated lupeolic acid suppresses the biosynthesis of eicosanoids through inhibition of cytosolic phospholipase A2. Biochemical Pharmacol, 84, 681-91

Golkowski, M., Pergola, C., Werz, O. and Ziegler, T. (2012) Strategy for catch and release of azide-tagged biomolecules utilizing a photolabile strained alkyne construct. Org Biomol Chem, 10, 4496-9

Banoglu, E., Çaliskan, B., Luderer, S., Eren, G., Özkan, Y., Altenhofen, W., Weinigel, C., Barz, D., Gerstmeier, J., Pergola, C. and Werz, O. (2012) Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP). Bioorg Med Chem, 20, 3728-41

Chini, M., De Simone, R., Bruno, I., Riccio, R., Dehm, F., Weinigel, C., Barz, D., Werz, O. and Bifulco, G. (2012) Design and Synthesis of a Second series of Triazole-based compounds as potent dual mPGES-1 and 5-Lipoxygenase inhibitors. Eur J Med Chem, 54, 311-23

Koeberle, S., Romir, J., Fischer, S., Koeberle, A., Schattel, V., Albrecht, W., Grütter, C., Werz, O., Rauh, D., Stehle, T. and Laufer, S. (2012) Skepinone-L is a selective p38 mitogen activated protein kinase (MAPK) inhibitor. Nat Chem Biol, 8, 141-3

Rossi, A., Dehm, F., Kiesselbach, C., Haunschild, J., Sautebin, L. and Werz, O. (2012) The novel Sinupret® dry extract exhibits anti-inflammatory effectiveness in vivo. Fitoterapia, 83, 715-20

Bauer, J., Kuehnl, S., Rollinger, J.M., Scherer, O., Northoff, H., Stuppner, H., Werz, O. and Koeberle, A. (2012) Carnosol and carnosic acids from Salvia officinalis inhibit microsomal prostaglandin E2 synthase-1. J Pharmaol Exp Ther, 342, 169-76

Skarke, C., Kuczka, K., Tausch, L., Werz, O., Rossmanith, T., Barrett, J., Harder, S., Holtmeier, W. and Schwarz, J. (2012) Increased bioavailability of 11 keto-beta-boswellic acid following single oral dose frankincense extract administration after a standardized meal in healthy male volunteers: Modeling and simulation considerations for evaluating drug exposures. J Clin Pharmacol, 52, 1592-600

Noha, S., Jazzar, B., Kuehnl, S., Rollinger, J.M., Stuppner, H., Schaible, A.M., Werz, O., Wolber, G., Schuster, D. (2012) Pharmacophore-based discovery of a novel cytosolic phospholipase A2α inhibitor. Bioorg Med Chem Lett, 22,1202-7

Klenner, A., Hähnke, V., Geppert, T., Schneider, P., Zettl, H., Haller, S., Rodrigues, T., Reisen, F., Hoy, B., Schaible, A., Werz, O., Wessler, S. and Schneider, G. (2012) From virtual screening to bioactive compounds by visualizing and clustering of chemical space. Mol Inf, 31, 21-26

Minassi, A., Cicione, L., Koeberle, A., Bauer, J., Laufer, S., Werz, O. and Appendino, G. (2012) A Multicomponent Carba-Betti Strategy to Alkylidene Heterodimers: Synthesis and Structure-Activity Relationships of Arzanol. Eur J Org Chem, 4, 772-779

Hörnig, M., Markoutsa, S., Häfner, A.-K., George, S., Wisniewska, J.M., Rödl, C.B., Hofmann, B., Maier, T., Karas, M., Werz, O. and Steinhilber, D. (2011) Inhibition of 5-lipoxygenase by U73122 is due to covalent binding to cysteine 416. Biochim Biophys Act, 1821, 279-86

Henkel, A., Kather, N., Mönch, B., Northoff, H., Jauch, J. and Werz, O. (2012) Boswellic acids from frankincense inhibit lipopolysaccharide functionality through direct molecular interference. Biochem Pharmacol, 83, 115-21
2011
Çalışkan, B., Luderer, S., Özkan, Y., Werz, O. and Banoglu, E. (2011) Pyrazol-3-propanoic acid derivatives as novel inhibitors of leukotriene biosynthesis in human neutrophils. Eur J Med Chem, 46, 5021-33

Hieke, M., Ness, J., Steri, R., Greiner, C., Werz, O., Schubert-Zsilavecz, M., Weggen, S. and Zettl, H. (2011) SAR studies of acidic dual γ-secretase/ PPARγ modulators. Bioorg Med Chem, 19, 5372-82

Pergola, C., Jazzar, B., Rossi, A., Northoff, H., Hamburger, M., Sautebin, L. and Werz, O. (2011) On the inhibition of 5-lipoxygenase product formation by tryptanthrin: mechanistic studies and efficiency in vivo. Br J Pharmacol, 165, 765-76

Baumgartner, L., Sosa, S., Atanasov, A., Widowitz, U., Fakhrudin, N., Bauer, J., Del Favero, G., Ponti, C., Heiss, E., Schwaiger, S., Ladurner, A., Della Loggia, R., Rollinger, J., Werz, O., Bauer, R., Dirsch, V., Tubaro, A. and Stuppner, H. (2011) Lignan Derivatives from Krameria lappacea Roots Inhibit Acute Inflammation in Vivo and Pro-inflammatory Mediators in Vitro. J Nat Prod,74, 1779-86

Pergola, C., Rogge, A., Dodt, D., Northoff, H., Weinigel, C., Barz, D., Rådmark, O., Sautebin, L. and Werz, O. (2011) Testosterone suppresses phospholipase D causing sex differences in leukotriene biosynthesis in human monocytes. FASEB Journal, 25, 3377-87

Greiner, C., Zettl, H., Koeberle, A., Pergola, C., Northoff, H., Schubert-Zsilavecz, M. and Werz, O. (2011) Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1. Bioorg Med Chem, 19, 3394-401

Hieke, M., Greiner, C., Dittrich, M., Reisen, F., Schneider, G., Schubert-Zsilavecz, M. and Werz, O. (2011) Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid. J Med Chem, 54, 4490-507

Koeberle, A., Rossi, A., Bauer, J., Dehm, F., Verotta, L., Northoff, H., Sautebin, L. and Werz, O. (2011) Hyperforin, an anti-inflammatory constituent from St. John's wort, inhibits microsomal prostaglandin E2 synthase-1 and suppresses prostaglandin E2 formation in vivo. Front Pharmacol, 2, 7

Pergola, C., Jazzar, B., Rossi, A., Buehring, U., Luderer, S., Dehm, F., Northoff, H., Sautebin, L. and Werz, O. (2011) Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent inhibitor of 5-lipoxygenase. J Pharmacol Exp Ther, 338, 205-13

Greiner, C., Hörnig, C., Rossi, A., Pergola, C., Zettl, H., Schubert-Zsilavecz, M., Steinhilber, D., Sautebin, L. and Werz, O. (2011) 2-(4-(Biphenyl-4-ylamino)-6-chloropyrimidin-2-ylthio)octanoic acid (HZ52) - a novel type 5-lipoxygenase inhibitor with favorable molecular pharmacology and efficacy in vivo. Br J Pharmacol, 164, 781-93

Waltenberger, B., Wiechmann, K., Bauer, J., Markt, P., Noha, S.M., Wolber, G., Rollinger, J.M., Werz, O., Schuster, D. and Stuppner, H. (2011) Pharmacophore Modeling and Virtual Screening for Novel Acidic Inhibitors of Microsomal Prostaglandin E2 Synthase-1 (mPGES-1). J Med Chem, 54, 3163-74

Hieke, M., Greiner, C., Thieme, T., Schubert-Zsilavecz, M., Werz, O. and Zettl, H. (2011) A novel class of dual mPGES-1/5-LO inhibitors based on the α-naphthyl-pirinixic acid scaffold. Bioorg Med Chem Lett, 21, 1329-33

De Simone, R., Chini, MG, Bruno, I., Riccio, R., Mueller, D., Werz, O. and Bifulco, G. (2011) Structure-based discovery of inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1, 5-lipoxygenase (5-LO) and 5-lipoxygenase-activating protein (FLAP): promising hits for the development of new anti-inflammatory agents. J Med Chem, 54, 1565-75

Bauer, J., Koeberle, A., Dehm, F., Pollastro, F., Appendino, G., Northoff, H., Rossi, A., Sautebin, L. and Werz, O. (2011) Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivo. Biochem Pharmacol, 81, 259-68

Gerbeth, K., Meins, J., Werz, O., Schubert-Zsilavecz, M. and Abdel-Tawab, M. (2011) Determination of myrtucommulone from Myrtus communis in human and rat plasma by liquid chromatography/tandem mass spectrometry. Planta Med, 77, 450-4

Siemoneit, U., Koeberle, A., Rossi, A., Dehm, F., Reckel, S., Maier, T.J., Jauch, L., Northoff, H., Bernhard, F., Doetsch, V., Sautebin, L. and Werz, O. (2011) Boswellic acids inhibit microsomal prostaglandin E2 synthase-1: A molecular basis for the anti-inflammatory actions of the bioactive ingredients from frankincense. Br J Pharmacol, 162, 147-62
2010 und früher
Hieke, M., Ness, J., Steri, R., Dittrich, M., Greiner, C., Werz, O., Baumann, K., Schubert-Zsilavecz, M., Weggen, S. and Zettl, H. (2010) Design, synthesis and biological evaluation of a novel class of γ-secretase modulators with PPARγ activity. J Med Chem, 53, 4691-700.

Müller, H., Paul, M., Hartmann, D., Huch, V., Blaesius, D., Koeberle, A., Werz, O. and Jauch, J. (2010) Totalsynthese von Myrtucommulon A. Angew Chem Int Ed Engl, 49, 2045-2049.

Steinbrink, SD., Pergola C., George, S., Metzner, J., Fischer, A., Häfner, A-K., Wisniewska, JM., Geisslinger, G., Werz, O., Steinhilber, D. and Maier, TJ. (2010) Sulindac sulfide suppresses 5-lipoxygenase at clinically relevant concentrations. Cell Moll Life Sci, 67, 797-806.

Hoffmann, M., Lopez, JJ, Feisst, C., Pawelczikc, S., Jakobsson, P.-J., Sorg, BL, Glaubitz, C., Steinhilber, D. and Werz, O. (2010) Hyperforin induces Ca2+-independent arachidonic acid release in human platelets by facilitating cytosolic phospholipase A2 activation through select phospholipid interactions. Biochim Biophys Acta, 1801, 462-472.

Geller, F., Schmidt,C., Göttert, M., Fronza, M., Schattel, V., Heinzmann, B., Werz, O., Flores, E. M.M., Merfort, I. and Laufer, S. (2010) Identification of rosmarinic acid as the major active constituent in Cordia Americana. J Ethnopharmacol, 128, 561-566.

Rossi, A., Pergola, C., Koeberle, A.,Bramanti, P., Cuzzocrea, S., Werz, O. and Sautebin, L. (2010) The 5-lipoxygenase inhibitor zileuton suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages. Br J Pharmacol, 161, 555-570

Pergola, C. and Werz, O. (2010) 5-Lipoxygenase modulators: a review of recent developments and patents. Exp Opin Ther Patents, 20, 355-375

Abdel-Tawab, M., Werz, O. and Schubert-Zsilavecz, M. (2010) Boswellia serrata: an overall assessment of in vitro, preclinical, pharmacokinetic and clinical data. Clin Pharmacokinet, in press

Rossi, A., Di Paola, R., Mazzon, E., Genovese, T., Caminiti, R., Bramanti, P., Pergola, C., Koeberle, A., Werz, O., Sautebin, L. and Cuzzocrea, S. (2009) Myrtucommulone from Myrtus communis exhibits potent anti-inflammatory effectiveness in vivo. J Pharmacol Exp Ther, 329, 76-86

Siemoneit, U., Pergola, C., Jazzar, B., Northoff, H. Skarke, C., Jauch, J. and Werz, O. (2009) On the interference of boswellic acids with 5-lipoxygenase: mechanistic studies in vitro and pharmacological relevance. Eur J Pharmacol, 606, 246-254.

Koeberle, A., Siemoneit, U., Northoff, H., Hofmann, B., Schneider, G. and Werz, O. (2009) MK-886, an inhibitor of the 5-lipoxygenase-activating protein, inhibits cyclooxygenase-1 activity and suppresses platelet aggregation. Eur J Pharmacol, 608, 84-90

Koeberle, A., Northoff, H. and Werz, O. (2009) Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol. Biochem Pharmacol, 77, 1513-1521

Koeberle, A., Pollastro, F., Northoff, H. and Werz, O. (2009) Myrtucommulone, a natural acylphloroglucinol, inhibits microsomal prostaglandin E2 synthase-1. Br J Pharmacol, 156, 952-961.

Karg, E.-M., Luderer, S., Pergola, C., Buehring, U., Rossi, A., Northoff, H., Sautebin, L., Troschütz, R. and Werz, O. (2009) Structural optimization of 2-substituted alkyl 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase. J Med Chem, 52, 3474-3483

Feißt, C., Pergola, C., Koeberle, A., Dodt, G., Rakonjac, M., Hoffmann, M., Hoernig, C., Fischer, L., Steinhilber, D., Rådmark, O., Franke, L., Schneider, G. and Werz, O. (2009) Hyperforin inhibits 5-lipoxygenase by interference with the C2-like domain. Cell Moll Life Sci, 66, 2759-2771

Koeberle, A., Northoff, H. and Werz, O. (2009) Curcumin blocks prostaglandin E2 biosynthesis through direct inhibition of the microsomal prostaglandin E2 synthase-1. Mol Cancer Ther, 8, 2348-2355

Liedtke, A.J., Keck, P.W.E.F., Lehmann, F., Koeberle, A., Werz, O. and Laufer, S.A. (2009) Arylpyrrolizidines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-LOX. J Med Chem, 52, 4968-4972.

Tausch, L., Henkel, A., Siemoneit, U., Poeckel, D., Kather, N., Franke, L., Schneider, G., Angioni, C., Geisslinger, G., Skarke, C., Holtmeier, W., Beckhaus, T., Karas, M., Jauch, J. and Werz, O. (2009) Identification of human cathepsin G as a functional target of boswellic acids from the anti-inflammatory remedy frankincense. J Immunol, 183, 3433-3442.

Koeberle, A., Bauer, J., Verhoff, M., Hoffmann, M., Northoff, H. and Werz, O. (2009) Green tea epigallocatechin-3-gallate inhibits microsomal prostaglandin E2 synthase-1. Biochem Biophys Res Commun, 388, 350-354.

Poeckel, D., Popescu, L., Rau, O., Schubert-Zsilavecz, M. and Werz, O. (2009) Immediate anti-inflammatory effects of novel pirinixic acid derivatives in activated human polymorphonuclear leukocytes. Eur J Pharmacol, 619,1-7

Koeberle, A., Karg, E.-M., Rossi, A., Dehm, F., Troschuetz, R., Sautebin, L. and Werz, O. (2009) Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E2 synthase-1. Bioorg Med Chem, 17, 7924-7932

Koeberle, A., Rossi, A., Zettl, H., Pergola, C., Dehm, F., Bauer, J., Greiner, C., Reckel, S., Hoernig, C., Northoff, H., Bernhard, F., Dötsch, V., Schubert-Zsilavecz, M., Sautebin, L. and Werz, O.(2009) The molecular pharmacology and in vivo activity of YS121 {2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid}, a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Pharmacol Exp Ther, 332, 840-848

Koeberle, A. and Werz, O. (2009) Inhibitors of the microsomal prostaglandin E2 synthase-1 as alternative to non steroidal anti-inflammatory drugs (NSAIDs) - a critical review. Current Med Chem,16, 4274-4296

Tretiakova, I., Blaesius, D., Maxia, L., Wesselborg, S., Schulze-Osthoff, K., Cinatl, J., Michaelis, M. and Werz, O. (2008) Myrtucommulone from Myrtus communis induces apoptosis in cancer cells via the mitochondrial pathway involving caspase-9. Apoptosis, 13,119-131
Siemoneit, U., Hofmann, B., Kather, N., Franke, L., Schneider, G., Jauch, J., Poeckel, D. and Werz, O. (2008) Boswellic acids interact with cyclooxygenases and inhibit cyclooxygenase activity. Biochem Pharmacol, 75, 503-513

Herb, F., Thye, T., Niemann, S., Browne, E.N.L., Chinbuah, M.A., Gyapong, J., Osei, I., Owusu-Dabo, E., Werz, O., Rüsch-Gerdes, S., Horstmann, R.D. and Meyer, C.G. (2008) ALOX5 variants associated with susceptibility to pulmonary tuberculosis. Hum Mol Genet, 17, 1052-1060

Albert, D., Pergola, C., Koeberle, A., Dodt, G., Steinhilber, D. and Werz, O. (2008) The role of diacylglyceride generation by phospholipase D and phosphatidic acid phosphatase in the activation of 5-lipoxygenase in polymorphonuclear leukocytes. J Leuk Biol, 83:1019-1027
Michel, A., Steinhilber, D. and Werz, O. (2008) Development of a method for expression and purification of the regulatory C2-like domain of human 5-lipoxygenase. Protein Expr Purif, 59, 110-116

Poeckel, D., Greiner, C., Verhoff, M., Rau, O., Tausch, L., Hörnig, L., Steinhilber, D., Schubert-Zsilavecz, M. and Werz, O. (2008) Carnosic acid and carnosol potently inhibit human 5-lipoxygenase and suppress pro-inflammatory responses of stimulated human polymorphonuclear leukocytes. Biochem Pharmacol, 76, 91-97

Koeberle, A., Siemoneit, U., Bühring, U., Northoff, H., Laufer, S., Albrecht, W. and Werz, O. (2008) Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1. J Pharmacol Exp Ther, 326, 975-982

Werz, O., Greiner, C., Koeberle, A., Hoernig, C., George, S., Popescu, L., Syha, I., Schubert-Zsilavecz, M. and Steinhilber, D. (2008) Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid. J Med Chem, 51, 5449-5453

Maier, T.J., Tausch, L., Hoernig, M., Coste, O., Schmidt, R., Angioni, C., Metzner, J., Groesch, S., Steinhilber, D., Werz, O. and Geisslinger, G. (2008) Celecoxib inhibits 5-lipoxygenase in vitro and in vivo. Biochem Pharmacol, 76, 862-872

Pergola, C., Dodt, G., Rossi, A., Neunhoeffer, E., Lawrenz, B., Hinnak, H., Samuelsson, B., Rådmark, O., Sautebin, L. and Werz, O. (2008) ERK-Mediated Regulation of Leukotriene Biosynthesis by Androgens: A Molecular Basis for Gender Differences in Inflammation and Asthma. Proc Natl Acad Sci USA, 105,19881-19886

Koeberle, A., Zettl, H., Greiner, C., Wurglics, M., Schubert-Zsilavecz, M. and Werz, O. (2008) Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase and 5-lipoxygenase. J Med Chem, 51, 8068-8076

Franke, L., Schwarz, O., Müller-Kuhrt, L., Hoernig, C., Fischer, L., George, S., Tanrikulu, Y., Schneider, P., Werz, O., Steinhilber, D., and Schneider, G. (2007) Identification of novel natural product-derived inhibitors of 5-lipoxygenase (5-LO) activity by ligand-based virtual screening, J. Med. Chem. 50, 2640-2646

Lechtken, A., Hörnig, M., Werz, O., Corvey, N., Zündorf, I., Dingermann, T., Brandes, R. and Steinhilber, D. (2007) Extracellular signal regulated kinase phosphorylates RORα4 at Thr-128 in vitro. Biochem Biophys Res Commun, 358, 890-896

Fischer, L., Hornig, M., Pergola, C., Meindl, N., Franke, L., Tanrikulu, Y., Dodt, G., Schneider, G., Steinhilber, D. and Werz, O. (2007) On the molecular mechanism of leukotriene synthesis inhibition by licofelone: the 5-lipoxygenase-activating protein as a molecular target. Br J Pharmacol, 152:471-480

Rådmark, O., Werz, O., Steinhilber D. and Samuelsson, B. (2007) 5-Lipoxygenase: Regulation of expression and enzyme activity (Invited Review). Trends Biochem Sci, 32, 332-341

Werz, O. (2007) Inhibition of 5-lipoxygenase product synthesis by natural compounds of plant origin (Invited Review). Planta Med, 73,1331-1357

Michaelis, M., Suhan, T., Michaelis, U.R., Beek, K., Rothweiler, F., Tausch, L., Werz, O., Eikel, D., Zörnig, M., Nau, H., Fleming, I., Doerr, H.W. and Cinatl jr., J. (2006) Valproic acid induces extracellular signal-regulated kinase 1/2 activation and inhibits apoptosis in endothelial cells. Cell Death Differ, 13, 446-53

Poeckel, D., Tausch, L., George, S., Jauch, J. and Werz, O. (2006) 3-O-Acetyl-11-keto-boswellic acid decreases basal intracellular Ca2+ levels and inhibits agonist-induced Ca2+ mobilisation and MAP kinase activation in human monocytes. J. Pharmacol Exp Ther, 316, 224-32

Dishard, D., Schnur, N., Klan, N., Werz, O. Steinhilber, D., Samuelsson, B. and Rådmark, O. (2006) Transcription factor Sp1 conveys basal, but not upregulated, 5-lipoxygenase gene expression in Mono Mac 6 cells. Biochim Biophys Acta, 1738, 37-47

Aleksandrov, D. A., Zagryagskaya, A. N., Pushkareva, M. A., Sud'ina, G. F., Bachschmid, M., Peters-Golden, M., Werz, O. and Steinhilber, D. (2006) Cholesterol and its anionic derivatives inhibit 5-lipoxygenase activation in polymorphonuclear leukocytes and MonoMac6 cells. FEBS Journal, 273, 548-57

Sorg, B., Klan, N., Seuter, S., Dishard, D., Rådmark, D., Habenicht, A., Carlberg, C., Werz, O. and Steinhilber, D. (2006) Analysis of the 5-lipoxygenase promoter and characterization of a vitamin D receptor binding site. Biochim Biophys Acta, 1761, 686-697
Landwehr, J., George, S., Karg, E.M., Poeckel, D., Steinhilber, D., Troschuetz, R. and Werz, O. (2006) Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase. J Med Chem, 49, 4327-4332

Poeckel, D., Tausch, L., Kather, L., Jauch, J. and Werz, O. (2006) Boswellic acids stimulate arachidonic acid release and 12-lipoxygenase activity in human platelets independent of Ca2+ and differentially interact with platelet-type 12-lipoxygenase. Mol Pharmacol, 70, 1071-1078

Rakonjac, M., Fischer, L., Provost, P., Werz, O., Steinhilber, D., Samuelsson, B. and Rådmark, O. (2006) Coactosin-like protein supports 5-lipoxygenase enzyme activity and upregulates leukotriene A4 production. Proc Natl Acad Sci USA, 103, 13150-13155

Poeckel, D., Niedermeyer, T. H. J., Pham, H T. L., Mikolasch, A., Mundt, S., Lindequist, U., Lalk, M. and Werz, O. (2006) Inhibition of human 5-lipoxygenase and anti-neoplastic effects by 2-amino-1,4-benzoquinones. Medicinal Chemistry, 2, 591-595

Peifer, C., Werz, O., Poeckel, D., Schollmeyer, D. and Laufer, S. (2006) (4R)-4-Hydroxy-1-[(2S)-2-hydroxydodecyl]-L-Proline monohydrate. Acta Cryst E, 62: O5138-O5140 Part 11

Poeckel, D. and Werz, O. (2006) Boswellic acids: biological actions and molecular targets (Invited Review). Current Med Chem, 28, 3359-3369

Werz, O. and Steinhilber D. (2006) Therapeutic options for 5-lipoxygenase inhibitors (Invited Review). Pharmacol & Ther, 112, 701-718

Feißt, C., Albert, D., Verotta, L. and Werz, O. (2005) Evaluation of hyperforin analogues for inhibition of 5-lipoxygenase, Medicinal Chemistry, 1, 287-291

Feißt, C., Albert, D., Steinhilber, D. and Werz, O. (2005) The aminosteroid phospholipase C antagonist U-73122 potently inhibits 5-lipoxygenase in vivo and in vitro. Mol Pharmacol, 67, 1751-1757
Hornig, C., Albert, D., Fischer, L., Hornig, M., Radmark, O., Steinhilber, D. and Werz, O. (2005) 1-Oleoyl-2-acetylglycerol stimulates 5-lipoxygenase activity via a putative (phospho)lipid-binding site within the N-terminal C2-like domain. J Biol Chem, 280, 26913-26921

Feißt, C., Franke, L., Appendino, G. and Werz, O. (2005) Identification of molecular targets of the oligomeric non-prenylated acylphloroglucinols from Myrtus communis and their implication as anti-inflammatory compounds. J Pharmacol Exp Ther, 315, 389-396
Poeckel, D., Tausch, L., Altmann, A., Feißt, C., Klinkhardt, U., Graff, J., Harder, S. and Werz, O. (2005) Induction of central signaling pathways and select functional effects in human platelets by ß-boswellic acid. Br J Pharmacol, 146, 514-524.

Werz, O., Tretiakova, I., Michel, A., Ulke-Lemee, A., Hörnig, M., Franke, L., Schneider, G., Samuelsson, B., Rådmark, O. and Steinhilber, D. (2005) Caspase-mediated degradation of human 5-lipoxygenase in B-lymphocytic cells. Proc Natl Acad Sci USA, 102, 13164-13169

Fischer, L., Poeckel, D., Buerkert, E., Steinhilber, D. and Werz, O. (2005) Inhibitors of actin polymerisation stimulate arachidonic acid release and 5-lipoxygenase activation by upregulation of Ca2+ mobilisation in polymorphonuclear leukocytes involving Src family kinases. Biochim Biophys Acta, 1736, 109-119.

Franke, L., Byvatov, E., Werz, O., Steinhilber, D., Schneider P. and Schneider, G. (2005) Extraction and visualization of pharmacophore models using Support-Vector-Machines. J Med Chem, 48, 6997-7004.

Werz, O. and Steinhilber D. (2005) Development of 5-lipoxygenase inhibitors - Lessons from cellular enzyme regulation. Biochemical Pharmacol, 70, 327-323

Werz, O. and Steinhilber D. (2005) Pharmacological intervention with 5-lipoxygenase: new insights and novel compounds. Exp Opin Ther Patents, 15, 505-519

Altmann, A., Poeckel, D., Fischer, L., Schubert-Zsilavecs, M., Steinhilber, D. and Werz, O. (2004) Coupling of boswellic acid-induced Ca2+-mobilization and MAPK activation to lipid metabolism and peroxide formation in human leukocytes. Br J Pharmacol, 141, 223-232

Feißt, C. and Werz, O. (2004) Suppression of receptor-coupled calcium mobilization and functional leukocyte responses by hyperforin. Biochem. Pharmacol. 67, 1531-1539

Fischer, L., Steinhilber, D. and Werz, O. (2004) Molecular pharmacological profile of the nonredox-type 5-lipoxygenase inhibitor CJ-13,610. Br J Pharmacol,142(5), 861-868.

Werz, O. (2004) 5-Lipoxygenase: regulation and pharmacology (Invited Review). Medicinal Chemistry Reviews-Online, 1 (1), 201-223.

Werz, O., Bürkert, E., Fischer, L., Szellas, D., Dishart, D., Samuelsson, B., Rådmark, O. and Steinhilber, D. (2003) 5-Lipoxygenase activation by MAPKAPK-2 and ERKs. Adv Exp Med Biol, 525, 129-132.

Bürkert, E., Szellas, D., Rådmark, O., Steinhilber, D. and Werz, O. (2003) Cell type-specific activation of 5-lipoxygenase by arachidonic acid. J Leuk Biol, 73, 191-200

Fischer, L., Szellas, D., Rådmark, O., Steinhilber, D. and Werz, O. (2003) Phosphorylation and stimulus-dependent inhibition of cellular 5-lipoxygenase activity by nonredox-type inhibitors. FASEB Journal,17, 949-951

Albert, D., Bürkert, E., Steinhilber, D. and Werz, O. (2003) Induction of 5-lipoxygenase activation in polymorphonuclear leukocytes by 1-oleoyl-2-acetylglycerol. Biochim Biophys Acta, 1631, 85-93

Klan, N., Uhl, J., Rose, M., Entian, K.-D., Werz, O. and Steinhilber, D. (2003) DNA methylation regulates 5-lipoxygenase promoter activity. Adv. Exp. Med. Biol. 525, 169-172

Bürkert, E., Arnold, C., Hammarberg, T., Rådmark, O., Steinhilber, D. and Werz, O. (2003) The C2-like β-barrel domain mediates the Ca2+-dependent resistance of 5-lipoxygenase activity against inhibition by glutathione peroxidase-1. J Biol Chem, 278, 42846-42853

Werz, O., Bürkert, E., Samuelsson, B., Rådmark, O. and Steinhilber, D. (2002) Activation of 5-lipoxygenase by cell stress is calcium-independent in human polymorphonuclear leukocytes. Blood, 99 (3), 1044-1052.

Uhl, J., Klan, N., Rose, M., Entian, K.-D., Werz, O. and Steinhilber, D. (2002) The 5-lipoxygenase promotor is regulated by methylation. J Biol Chem, 277, 4374-4379.

Altmann, A., Fischer, L., Schubert-Zsilavecs, M., Steinhilber, D. and Werz, O. (2002) Boswellic acids activate p42MAPK and p38 MAPK and stimulate the mobilisation of calcium. Biochem Biophys Res Commun, 190, 185-190.

Bürkert, E., Samuelsson, B., Rådmark, O., Steinhilber, D. and Werz, O. (2002) Hypertonicity suppresses ionophore-induced product formation and translocation of 5-lipoxygenase in leukocytes. J Leuk Biol, 71, 477-486.

Werz, O., Szellas, D., Steinhilber, D. and Rådmark, O. (2002) Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPKAP kinase 2. J Biol Chem, 277, 14793-14800.

Werz, O., Bürkert, E., Fischer, L., Szellas, D., Dishart, D., Samuelsson, B., Rådmark, O. and Steinhilber, D. (2002) Extracellular signal-regulated kinases phosphorylate 5-lipoxygenase and stimulate 5-lipoxygenase product formation in leukocytes. FASEB Journal, 16, 1441-1443.

Bürkert, E., Steinhilber, D. and Werz, O. (2002) Monocyte-derived soluble protein confers 5-lipoxygenase activity Ca2+-dependent. Biochem Biophys Res Commun, 295(4), 985-991.

Albert, D., Zündorf, I., Dingermann,T., Müller, W. E., Steinhilber, D. and Werz, O. (2002) Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. Biochem Pharmacol, 64, 1767-1775

Werz, O. (2002) 5-Lipoxygenase: Cellular biology and molecular pharmacology (Invited Review). Curr Drug Targets Inflamm Allergy, 1 (1), 23-44.

Werz, O., Klemm, J., Samuelsson, B. and Rådmark, O. (2001) Phorbol ester upregulates capacities for nuclear translocation and phosphorylation of 5-lipoxygenase in Mono Mac 6 cells and human PMNL. Blood, 97, 2487-2495

Schumann, D., Werz, O., Szellas, D. and Steinhilber, D. (2001) Regulation of cellular 5-lipoxygenase activity by glutathione peroxidases. Adv. Prostagland. Thromboxane Leukotriene Res, 16, 21-23.

Werz, O., Klemm, J., Samuelsson, B. and Rådmark, O. (2001) Phosphorylation and activation of 5-lipoxygenase by p38 kinase activated MAPKAP kinases. Adv. Prostagland. Thromboxane Leukotriene Res, 16, 1-7.

Werz, O., Klemm, J., Rådmark, O. and Samuelsson, B. (2001) p38 MAP kinase mediates stress-induced leukotriene synthesis in a human B-lymphocyte cell line. J Leuk Biol,70, 830-838

Gaschott, T., Werz, O., Steinmeyer, A., Steinhilber, D. and Stein, J. (2001) Butyrate-induced differentiation of Caco-2 cells is mediated by vitamin D receptor. Biochem Biophys Res Commun, 288, 690-696

Werz, O., Szellas, D. and Steinhilber, D. (2000) Reactive oxygen species released from granulocytes stimulate 5- lipoxygenase activity in a B-lymphocytic cell line. Eur J Biochem, 267, 1263-9.

Werz, O., Wiesinger, H., Steinmeyer, A. and Steinhilber, D. (2000) New vitamin D receptor agonists with decreased metabolic stability. Biochem Pharmacol, 59, 1597-601.

Straif, D., Werz, O., Kellner, R., Bahr, U. and Steinhilber, D. (2000) Glutathione peroxidase-1 but not -4 is involved in the regulation of cellular 5-lipoxygenase activity in monocytic cells. Biochem J, 349, 455-461.

Werz, O., Klemm, J., Samuelsson, B. and Rådmark, O. (2000) 5-lipoxygenase is phosphorylated by p38 kinase-dependent MAPKAP kinases. Proc Natl Acad Sci USA,97, 5261-5266.

Werz, O. and Steinhilber, D. (1998) Regulation of 5-lipoxygenase activity by selenium-dependent peroxidases - effects of transforming growth factor-beta and 1,25-dihydroxyvitamin D3. Adv Exp Med Biol, 433, 383-6.

Werz, O., Szellas, D., Henseler, M. and Steinhilber, D. (1998) Nonredox 5-lipoxygenase inhibitors require glutathione peroxidase for efficient inhibition of 5-lipoxygenase activity. Mol Pharmacol, 54, 445-51.

Benz, M., Werz, O., Jacob, R. and Steinhilber, D. (1997) pH-dependent regulation of leukocyte 5-lipoxygenase activity in inflammatory exudates by albumin. Inflamm Res, 46, 366-72.

Werz, O., Schneider, N., Brungs, M., Sailer, E. R., Safayhi, H., Ammon, H. P. and Steinhilber, D. (1997) A test system for leukotriene synthesis inhibitors based on the in-vitro differentiation of the human leukemic cell lines HL-60 and Mono Mac 6. Naunyn Schmiedebergs Arch Pharmacol, 356, 441-5.

Werz, O. and Steinhilber, D. (1996) Selenium-dependent peroxidases suppress 5-lipoxygenase activity in B-lymphocytes and immature myeloid cells. The presence of peroxidase- insensitive 5-lipoxygenase activity in differentiated myeloid cells. Eur J Biochem, 242, 90-7.
Werz, O., Brungs, M. and Steinhilber, D. (1996) Purification of transforming growth factor beta 1 from human platelets. Pharmazie, 51, 893-6.

Steinhilber, D., Brungs, M., Werz, O., Wiesenberg, I., Danielsson, C., Kahlen, J. P., Nayeri, S., Schrader, M. and Carlberg, C. (1995) The nuclear receptor for melatonin represses 5-lipoxygenase gene expression in human B lymphocytes. J Biol Chem, 270, 7037-40.