{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,11]],"date-time":"2026-09-11T17:26:04Z","timestamp":1789147564390,"version":"build-2803163510"},"reference-count":20,"publisher":"Elsevier BV","issue":"6","license":[{"start":{"date-parts":[[2020,3,1]],"date-time":"2020-03-01T00:00:00Z","timestamp":1583020800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2020,3,1]],"date-time":"2020-03-01T00:00:00Z","timestamp":1583020800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic &amp; Medicinal Chemistry Letters"],"published-print":{"date-parts":[[2020,3]]},"DOI":"10.1016\/j.bmcl.2020.126967","type":"journal-article","created":{"date-parts":[[2020,1,14]],"date-time":"2020-01-14T20:37:44Z","timestamp":1579034264000},"page":"126967","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":12,"title":["A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor ROR\u03b3t"],"prefix":"10.1016","volume":"30","author":[{"given":"Xin","family":"Jiang","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Irina","family":"Dulubova","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Scott A.","family":"Reisman","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Martha","family":"Hotema","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chun-Yue I.","family":"Lee","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liping","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lyndsey","family":"McCauley","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Isaac","family":"Trevino","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Deborah A.","family":"Ferguson","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yigitcan","family":"Eken","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Angela K.","family":"Wilson","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"W. Christian","family":"Wigley","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Melean","family":"Visnick","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmcl.2020.126967_b0005","unstructured":"Djerassi C, Rosenkranz G, Kaufmann S, Paraki J, Romo J. US patent 2671092, 1954."},{"issue":"6","key":"10.1016\/j.bmcl.2020.126967_b0010","doi-asserted-by":"crossref","first-page":"641","DOI":"10.1038\/ni.1610","article-title":"The differentiation of human T(H)-17 cells requires transforming growth factor-beta and induction of the nuclear receptor RORgammat","volume":"9","author":"Manel","year":"2008","journal-title":"Nat Immunol."},{"issue":"10","key":"10.1016\/j.bmcl.2020.126967_b0015","doi-asserted-by":"crossref","first-page":"493","DOI":"10.1016\/j.tips.2014.07.006","article-title":"Targeting Th17 cells in autoimmune diseases","volume":"35","author":"Yang","year":"2014","journal-title":"Trends Pharmacol Sci."},{"issue":"1","key":"10.1016\/j.bmcl.2020.126967_b0020","doi-asserted-by":"crossref","first-page":"88","DOI":"10.1002\/cpt.893","article-title":"Anti-IL-23 and Anti-IL-17 Biologic Agents for the Treatment of Immune-Mediated Inflammatory Conditions","volume":"103","author":"Frieder","year":"2018","journal-title":"Clin Pharmacol Ther."},{"issue":"24","key":"10.1016\/j.bmcl.2020.126967_b0025","doi-asserted-by":"crossref","first-page":"10976","DOI":"10.1021\/acs.jmedchem.8b00588","article-title":"Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-gamma (RORgamma or RORc) Inhibitors: Hits and Misses","volume":"61","author":"Pandya","year":"2018","journal-title":"J Med Chem."},{"key":"10.1016\/j.bmcl.2020.126967_b0030","doi-asserted-by":"crossref","first-page":"8833","DOI":"10.1038\/ncomms9833","article-title":"Identification of an allosteric binding site for RORgammat inhibition","volume":"6","author":"Scheepstra","year":"2015","journal-title":"Nat Commun."},{"issue":"10","key":"10.1016\/j.bmcl.2020.126967_b0035","doi-asserted-by":"crossref","first-page":"1193","DOI":"10.1016\/j.chembiol.2016.06.017","article-title":"Bidirectional Allosteric Communication between the ATP-Binding Site and the Regulatory PIF Pocket in PDK1 Protein Kinase","volume":"23","author":"Schulze","year":"2016","journal-title":"Cell Chem Biol."},{"issue":"16","key":"10.1016\/j.bmcl.2020.126967_b0040","doi-asserted-by":"crossref","first-page":"4372","DOI":"10.1002\/anie.201707875","article-title":"The Cysteinome of Protein Kinases as a Target in Drug Development","volume":"57","author":"Chaikuad","year":"2018","journal-title":"Angew Chem Int Ed Engl."},{"key":"10.1016\/j.bmcl.2020.126967_b0045","doi-asserted-by":"crossref","first-page":"53","DOI":"10.2174\/978160805265311201010053","article-title":"Covalent interactions of organotins with nuclear receptors","author":"Grun","year":"2012","journal-title":"Biochem Biol Effects Organotins"},{"issue":"14","key":"10.1016\/j.bmcl.2020.126967_b0050","doi-asserted-by":"crossref","first-page":"14145","DOI":"10.1074\/jbc.M500901200","article-title":"Alpha, beta-unsaturated ketone is a core moiety of natural ligands for covalent binding to peroxisome proliferator-activated receptor gamma","volume":"280","author":"Shiraki","year":"2005","journal-title":"J Biol Chem."},{"key":"10.1016\/j.bmcl.2020.126967_b0055","first-page":"1","article-title":"HDX-MS reveals structural determinants for RORgamma hyperactivation by synthetic agonists","volume":"8","author":"Strutzenberg","year":"2019","journal-title":"Elife"},{"issue":"5","key":"10.1016\/j.bmcl.2020.126967_b0060","doi-asserted-by":"crossref","first-page":"923","DOI":"10.1210\/me.2009-0507","article-title":"Structural basis for hydroxycholesterols as natural ligands of orphan nuclear receptor RORgamma","volume":"24","author":"Jin","year":"2010","journal-title":"Mol Endocrinol."},{"issue":"4","key":"10.1016\/j.bmcl.2020.126967_b0065","doi-asserted-by":"crossref","first-page":"704","DOI":"10.1002\/prot.20660","article-title":"Very fast empirical prediction and rationalization of protein pKa values","volume":"61","author":"Li","year":"2005","journal-title":"Proteins"},{"key":"10.1016\/j.bmcl.2020.126967_b0070","unstructured":"Molecular Operating Environment (MOE), 2016.08. [computer program]. Chemical Computing Group ULC. Montreal, 2016."},{"issue":"23","key":"10.1016\/j.bmcl.2020.126967_b0075","doi-asserted-by":"crossref","first-page":"5802","DOI":"10.1016\/j.bmcl.2016.10.023","article-title":"Discovery of phenoxyindazoles and phenylthioindazoles as RORgamma inverse agonists","volume":"26","author":"Ouvry","year":"2016","journal-title":"Bioorg Med Chem Lett."},{"issue":"36","key":"10.1016\/j.bmcl.2020.126967_b0080","doi-asserted-by":"crossref","first-page":"9340","DOI":"10.1021\/bi00087a012","article-title":"Active site labeling of the Yersinia protein tyrosine phosphatase: the determination of the pKa of the active site cysteine and the function of the conserved histidine 402","volume":"32","author":"Zhang","year":"1993","journal-title":"Biochemistry"},{"issue":"10","key":"10.1016\/j.bmcl.2020.126967_b0085","doi-asserted-by":"crossref","first-page":"2674","DOI":"10.1021\/bi0620252","article-title":"Identification of catalytic cysteine, histidine, and lysine residues in Escherichia coli homoserine transsuccinylase","volume":"46","author":"Ziegler","year":"2007","journal-title":"Biochemistry"},{"issue":"52","key":"10.1016\/j.bmcl.2020.126967_b0090","doi-asserted-by":"crossref","first-page":"18673","DOI":"10.1073\/pnas.1413687112","article-title":"RORgammat-specific transcriptional interactomic inhibition suppresses autoimmunity associated with TH17 cells","volume":"111","author":"Park","year":"2014","journal-title":"Proc Natl Acad Sci USA"},{"issue":"4","key":"10.1016\/j.bmcl.2020.126967_b0095","doi-asserted-by":"crossref","first-page":"488","DOI":"10.3390\/ijms17040488","article-title":"RORC2 Genetic Variants and Serum Levels in Patients with Rheumatoid Arthritis","volume":"17","author":"Paradowska-Gorycka","year":"2016","journal-title":"Int J Mol Sci."},{"issue":"3","key":"10.1016\/j.bmcl.2020.126967_b0100","first-page":"564","article-title":"Assessment of murine collagen-induced arthritis by longitudinal non-invasive duplexed molecular optical imaging","volume":"55","author":"Scales","year":"2016","journal-title":"Rheumatology (Oxford)"}],"container-title":["Bioorganic &amp; Medicinal Chemistry Letters"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X20300202?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X20300202?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,18]],"date-time":"2025-10-18T07:32:40Z","timestamp":1760772760000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0960894X20300202"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2020,3]]},"references-count":20,"journal-issue":{"issue":"6","published-print":{"date-parts":[[2020,3]]}},"alternative-id":["S0960894X20300202"],"URL":"https:\/\/doi.org\/10.1016\/j.bmcl.2020.126967","relation":{},"ISSN":["0960-894X"],"issn-type":[{"value":"0960-894X","type":"print"}],"subject":[],"published":{"date-parts":[[2020,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor ROR\u03b3t","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry Letters","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmcl.2020.126967","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2020 Elsevier Ltd. All rights reserved.","name":"copyright","label":"Copyright"}],"article-number":"126967"}}