Publikationen von Prof. Dr. Oliver Werz

2019 Inhalt einblenden
  • 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, in press
  • 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, in press
  • 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., in press
  • Bartel K., Koeberle A., Schmitt S., Schulze A., Lengauer F., Werz O., Zischka H., Müller R., Menche D., Vollmar A.M., von Schwarzenberg K. (2019) Connecting lysosomes and mitochondria – a novel role for lipid metabolism in cancer cell death. Cell Commun Signal, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, 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, in press
  • 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., in press.
  • 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., in press
  • 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, in press
  • 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. in press
  • Shekfeh S., Çalışkan B., Fischer K., Yalçın T., Garscha U., Werz O., Banoglu E. (2019) A multi-step virtual screening protocol for identification of novel non-acidic microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors. ChemMedChem, 14(2):273-281
  • 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
2018 Inhalt einblenden

 

  • 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(1):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, in press.
  • Schexnaydre E.E., Gerstmeier J., Garscha U., Jordan P.J., Werz O., Newcomer M.E. (2018) A 5-Lipoxygenase-Specific Sequence Motif Impedes Enzyme Activity and Confers Dependence on a Partner Protein. Biochim Biophys Acta Mol Cell Biol Lipids, in press
  • 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(1):3834
  • 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.(2018) Melleolides from honey mushroom inhibit 5-lipoxygenase via Cys159. Cell Chem Biol, in press
  • Koeberle A., Werz O. (2018) Natural products as inhibitors of prostaglandin E2and pro-inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis.Biotechnol Adv., in press
  • 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
  • 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, in press
  • 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
  • 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., in press
  • 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, in press
  • Rettener J., Werner M., Meyer N., Werz O., Pohnert G. (2018) Survey of the C20 and C22 oxylipin family in marine diatoms. Tetrahedron lett., in press
2017 Inhalt einblenden
  • Glatzel D.K., Koeberle A., Pein H., Loeser K., Stark A., Keksel N., Werz O., Mueller R., Bischoff I., Fuerst R. (2017) Acetyl-CoAcarboxylase 1 regulates endothelial cell migration by shifting the phospholipid composition.J. Lipid Res., in press
  • 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. (2017) A Standardized Frankincense Extract Reduces Disease Activity in Relapsing-Remitting Multiple Sclerosis (The SABA phase IIa trial). J. Neurol. Neurosurg. Psychiatry, in press
  • 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. (2017) Drug-mediated intracellular donation of nitric oxide potently inhibits 5-lipoxygenase: a possible key to future anti-leukotriene therapy. Antioxid. Redox Signal., in press
  • 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, in press
  • 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, in press
  • 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, in press
  • Pace S., Sautebin L., Werz O. (2017) Sex-biased eicosanoid biology: impact for sex differences in inflammation and consequences for pharmacotherapy. Biochem Pharmacol, in press
  • 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, in press
  • 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., in press
  • 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 in the efficiency of leukotriene biosynthesis inhibitors. J Clin Invest, in press
  • 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, in press
  • 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 (2017) Docosahexaenoic acid in the treatment of rheumatoid arthritis: A double-blind, placebo-controlled, randomized cross-over study with microalgae vs. sunflower oil. Clin Nutr, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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, in press
  • 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
  • Schieferdecker S, König S, Pace S, Werz O*, Nett M* (2017) Myxochelin-Inspired 5-Lipoxygenase Inhibitors - Synthesis and Biological Evaluation. ChemMedChem, 12, 23-27
  • Bartel K., Winzi M., Ulrich M., Koeberle A., Menche D., Werz O., Müller R., Guck J., Vollmar A., von Schwarzenberg K. (2016) V-ATPase inhibition increases cancer cell stiffness and blocks membrane related Ras signaling - a new option for HCC therapy. Oncotarget, 8, 9476-9487
  • 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
  • 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
  • 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
  • Werz O., Gerstmeier J. Garscha U. (2017) Novel leukotriene biosynthesis inhibitors (2012-2016) as anti-inflammatory agents. Expert Opin Ther Pat, in press
2016 Inhalt einblenden
  • 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
  • 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
  • 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
  • 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 
  • 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
  • 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, in press
  • 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
    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
  • 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
  • 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
    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
  • 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
  • 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
  • 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, 7, 42751
  • 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
  • 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
  • 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
  • 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
  • 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
2015 Inhalt einblenden
  • 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 Inhalt einblenden
  • 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 Inhalt einblenden
  • 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 Inhalt einblenden
  • 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 Inhalt einblenden
  • 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 Inhalt einblenden
  • 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.
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