{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,23]],"date-time":"2026-09-23T14:19:57Z","timestamp":1790173197211,"version":"4.1.0"},"reference-count":34,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2018,8,1]],"date-time":"2018-08-01T00:00:00Z","timestamp":1533081600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"}],"funder":[{"name":"Deutsche Forschgungsgemeinschaft","award":["SFB1127"],"award-info":[{"award-number":["SFB1127"]}]},{"name":"Deutsche Forschgungsgemeinschaft","award":["SFB1278"],"award-info":[{"award-number":["SFB1278"]}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2018,8]]},"DOI":"10.1016\/j.ejmech.2018.07.031","type":"journal-article","created":{"date-parts":[[2018,7,24]],"date-time":"2018-07-24T22:14:17Z","timestamp":1532470457000},"page":"815-830","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":20,"special_numbering":"C","title":["Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation"],"prefix":"10.1016","volume":"156","author":[{"given":"Sun-Yee","family":"Cheung","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Markus","family":"Werner","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lucia","family":"Esposito","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fabiana","family":"Troisi","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vincenza","family":"Cantone","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stefanie","family":"Liening","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stefanie","family":"K\u00f6nig","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jana","family":"Gerstmeier","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andreas","family":"Koeberle","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rossella","family":"Bilancia","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Roberta","family":"Rizza","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3237-2584","authenticated-orcid":false,"given":"Antonietta","family":"Rossi","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fiorentina","family":"Roviezzo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Veronika","family":"Temml","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9933-8938","authenticated-orcid":false,"given":"Daniela","family":"Schuster","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hermann","family":"Stuppner","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Manfred","family":"Schubert-Zsilavecz","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Oliver","family":"Werz","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Thomas","family":"Hanke","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Simona","family":"Pace","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2018.07.031_bib1","doi-asserted-by":"crossref","first-page":"331","DOI":"10.1016\/j.bbalip.2014.08.012","article-title":"5-Lipoxygenase, a key enzyme for leukotriene biosynthesis in health and disease","volume":"1851","author":"Radmark","year":"2015","journal-title":"Biochim. Biophys. Acta"},{"key":"10.1016\/j.ejmech.2018.07.031_bib2","doi-asserted-by":"crossref","first-page":"5970","DOI":"10.1021\/acs.jmedchem.5b01750","article-title":"Design and development of microsomal prostaglandin E2 Synthase-1 inhibitors: challenges and future directions","volume":"59","author":"Koeberle","year":"2016","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib3","doi-asserted-by":"crossref","first-page":"1841","DOI":"10.1056\/NEJMra071371","article-title":"Leukotrienes","volume":"357","author":"Peters-Golden","year":"2007","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2018.07.031_bib4","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/j.bcp.2015.06.022","article-title":"Perspective of microsomal prostaglandin E2 synthase-1 as drug target in inflammation-related disorders","volume":"98","author":"Koeberle","year":"2015","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.ejmech.2018.07.031_bib5","doi-asserted-by":"crossref","first-page":"3","DOI":"10.1007\/1-4020-5688-5_1","article-title":"Anti-inflammatory drugs in the 21st century","volume":"42","author":"Rainsford","year":"2007","journal-title":"Subcell. Biochem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib6","doi-asserted-by":"crossref","first-page":"5","DOI":"10.1111\/j.1365-2796.2010.02246.x","article-title":"Microsomal prostaglandin E synthase-1 and 5- lipoxygenase: potential drug targets in cancer","volume":"268","author":"Radmark","year":"2010","journal-title":"J.\u00a0Intern. Med."},{"key":"10.1016\/j.ejmech.2018.07.031_bib7","doi-asserted-by":"crossref","DOI":"10.1016\/j.biotechadv.2018.02.010","article-title":"Natural products as inhibitors of prostaglandin E2 and pro- inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis","author":"Koeberle","year":"2018","journal-title":"Biotechnol. Adv."},{"key":"10.1016\/j.ejmech.2018.07.031_bib8","doi-asserted-by":"crossref","first-page":"1585","DOI":"10.1039\/c2mb05503a","article-title":"Dynamic eicosanoid responses upon different inhibitor and combination treatments on the arachidonic acid metabolic network","volume":"8","author":"He","year":"2012","journal-title":"Mol. Biosyst."},{"key":"10.1016\/j.ejmech.2018.07.031_bib9","doi-asserted-by":"crossref","DOI":"10.1172\/jci.insight.87031","article-title":"A\u00a0broad-spectrum lipidomics screen of antiinflammatory drug combinations in human blood","volume":"1","author":"Mazaleuskaya","year":"2016","journal-title":"JCI Insight"},{"key":"10.1016\/j.ejmech.2018.07.031_bib10","doi-asserted-by":"crossref","first-page":"3163","DOI":"10.1021\/jm101309g","article-title":"Pharmacophore modeling and virtual screening for novel acidic inhibitors of microsomal prostaglandin E(2) synthase-1 (mPGES-1)","volume":"54","author":"Waltenberger","year":"2011","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib11","doi-asserted-by":"crossref","first-page":"8958","DOI":"10.1021\/jm3010543","article-title":"Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX","volume":"55","author":"Elkady","year":"2012","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib12","doi-asserted-by":"crossref","first-page":"2034","DOI":"10.1021\/cg500157x","article-title":"Crystallizing membrane proteins in the lipidic mesophase. Experience with human prostaglandin E2 synthase 1 and an evolving strategy","volume":"14","author":"Li","year":"2014","journal-title":"Cryst. Growth Des."},{"key":"10.1016\/j.ejmech.2018.07.031_bib13","doi-asserted-by":"crossref","first-page":"217","DOI":"10.1126\/science.1197203","article-title":"The structure of human 5-lipoxygenase","volume":"331","author":"Gilbert","year":"2011","journal-title":"Science"},{"key":"10.1016\/j.ejmech.2018.07.031_bib14","doi-asserted-by":"crossref","first-page":"276","DOI":"10.1096\/fj.15-278010","article-title":"Time- resolved in situ assembly of the leukotriene-synthetic 5-lipoxygenase\/5-lipoxygenase- activating protein complex in blood leukocytes","volume":"30","author":"Gerstmeier","year":"2016","journal-title":"Faseb. J."},{"key":"10.1016\/j.ejmech.2018.07.031_bib15","doi-asserted-by":"crossref","first-page":"17","DOI":"10.1016\/j.bcp.2016.08.023","article-title":"BRP-187: a potent inhibitor of leukotriene biosynthesis that acts through impeding the dynamic 5-lipoxygenase\/5-lipoxygenase-activating protein (FLAP) complex assembly","volume":"119","author":"Garscha","year":"2016","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.ejmech.2018.07.031_bib16","doi-asserted-by":"crossref","first-page":"607","DOI":"10.1080\/13543776.2017.1276568","article-title":"Novel leukotriene biosynthesis inhibitors (2012-2016) as anti-inflammatory agents","volume":"27","author":"Werz","year":"2017","journal-title":"Expert Opin. Ther. Pat."},{"key":"10.1016\/j.ejmech.2018.07.031_bib17","doi-asserted-by":"crossref","first-page":"2961","DOI":"10.1016\/j.bbagen.2014.05.016","article-title":"An experimental cell-based model for studying the cell biology and molecular pharmacology of 5-lipoxygenase- activating protein in leukotriene biosynthesis","volume":"1840","author":"Gerstmeier","year":"2014","journal-title":"Biochim. Biophys. Acta"},{"key":"10.1016\/j.ejmech.2018.07.031_bib18","doi-asserted-by":"crossref","first-page":"59","DOI":"10.1038\/s41467-017-02538-5","article-title":"Human macrophages differentially produce specific resolvin or leukotriene signals that depend on bacterial pathogenicity","volume":"9","author":"Werz","year":"2018","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2018.07.031_bib19","doi-asserted-by":"crossref","first-page":"60","DOI":"10.1016\/j.bcp.2016.04.019","article-title":"The 5-lipoxygenase inhibitor RF-22c potently suppresses leukotriene biosynthesis in cellulo and blocks bronchoconstriction and inflammation in\u00a0vivo","volume":"112","author":"Schaible","year":"2016","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.ejmech.2018.07.031_bib20","doi-asserted-by":"crossref","first-page":"9398","DOI":"10.1038\/s41598-017-09795-w","article-title":"Pharmacological profile and efficiency in\u00a0vivo of diflapolin, the first dual inhibitor of 5-lipoxygenase-activating protein and soluble epoxide hydrolase","volume":"7","author":"Garscha","year":"2017","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2018.07.031_bib21","doi-asserted-by":"crossref","first-page":"1497","DOI":"10.1111\/bph.13545","article-title":"Anti-inflammatory and analgesic activity of carnosol and carnosic acid in\u00a0vivo and in\u00a0vitro and in silico analysis of their target interactions","volume":"174","author":"Maione","year":"2017","journal-title":"Br. J. Pharmacol."},{"key":"10.1016\/j.ejmech.2018.07.031_bib22","doi-asserted-by":"crossref","first-page":"612","DOI":"10.1002\/cmdc.201500598","article-title":"Structure-based design of microsomal prostaglandin E2 Synthase-1 (mPGES-1) inhibitors using a virtual fragment growing optimization scheme","volume":"11","author":"Lauro","year":"2016","journal-title":"ChemMedChem"},{"key":"10.1016\/j.ejmech.2018.07.031_bib23","doi-asserted-by":"crossref","first-page":"7874","DOI":"10.1016\/j.bmc.2013.10.006","article-title":"Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1","volume":"21","author":"Hanke","year":"2013","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib24","doi-asserted-by":"crossref","first-page":"2535","DOI":"10.1016\/j.bmc.2012.02.055","article-title":"Synthesis of new sulfonamides as lipoxygenase inhibitors","volume":"20","author":"Mustafa","year":"2012","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib25","doi-asserted-by":"crossref","first-page":"9031","DOI":"10.1021\/jm401557w","article-title":"Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in\u00a0vivo","volume":"56","author":"Hanke","year":"2013","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib26","doi-asserted-by":"crossref","first-page":"572","DOI":"10.1021\/ci100031x","article-title":"Conformer generation with OMEGA: algorithm and validation using high quality structures from the Protein Databank and Cambridge Structural Database","volume":"50","author":"Hawkins","year":"2010","journal-title":"J.\u00a0Chem. Inf. Model."},{"key":"10.1016\/j.ejmech.2018.07.031_bib27","doi-asserted-by":"crossref","first-page":"727","DOI":"10.1006\/jmbi.1996.0897","article-title":"Development and validation of a genetic algorithm for flexible docking","volume":"267","author":"Jones","year":"1997","journal-title":"J.\u00a0Mol. Biol."},{"key":"10.1016\/j.ejmech.2018.07.031_bib28","doi-asserted-by":"crossref","first-page":"715","DOI":"10.1016\/j.ejmech.2016.10.046","article-title":"Optimization of benzoquinone and hydroquinone derivatives as potent inhibitors of human 5-lipoxygenase","volume":"127","author":"Peduto","year":"2017","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib29","doi-asserted-by":"crossref","first-page":"3167","DOI":"10.1172\/JCI92885","article-title":"Androgen-mediated sex bias impairs efficiency of leukotriene biosynthesis inhibitors in males","volume":"127","author":"Pace","year":"2017","journal-title":"J.\u00a0Clin. Invest."},{"key":"10.1016\/j.ejmech.2018.07.031_bib30","doi-asserted-by":"crossref","first-page":"8068","DOI":"10.1021\/jm801085s","article-title":"Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase","volume":"51","author":"Koeberle","year":"2008","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2018.07.031_bib31","doi-asserted-by":"crossref","first-page":"949","DOI":"10.1096\/fj.02-0815fje","article-title":"Phosphorylation- and stimulus-dependent inhibition of cellular 5-lipoxygenase activity by nonredox-type inhibitors","volume":"17","author":"Fischer","year":"2003","journal-title":"Faseb. J."},{"key":"10.1016\/j.ejmech.2018.07.031_bib32","doi-asserted-by":"crossref","first-page":"361","DOI":"10.1016\/S0378-4347(00)82742-5","article-title":"Separation of lipoxins and leukotrienes from human granulocytes by high-performance liquid chromatography with a Radial-Pak cartridge after extraction with an octadecyl reversed-phase column","volume":"493","author":"Steinhilber","year":"1989","journal-title":"J.\u00a0Chromatogr. A"},{"key":"10.1016\/j.ejmech.2018.07.031_bib33","doi-asserted-by":"crossref","first-page":"1577","DOI":"10.1111\/j.1476-5381.2010.00872.x","article-title":"Animal research: reporting in\u00a0vivo experiments: the ARRIVE guidelines","volume":"160","author":"Kilkenny","year":"2010","journal-title":"Br. J. Pharmacol."},{"key":"10.1016\/j.ejmech.2018.07.031_bib34","doi-asserted-by":"crossref","first-page":"1573","DOI":"10.1111\/j.1476-5381.2010.00873.x","article-title":"Guidelines for reporting experiments involving animals: the ARRIVE guidelines","volume":"160","author":"McGrath","year":"2010","journal-title":"Br. J. Pharmacol."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523418305877?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523418305877?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2024,7,8]],"date-time":"2024-07-08T12:08:47Z","timestamp":1720440527000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523418305877"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2018,8]]},"references-count":34,"alternative-id":["S0223523418305877"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2018.07.031","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2018,8]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2018.07.031","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2018 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}]}}