| Literature DB >> 25453817 |
Monique B van Niel1, Benjamin P Fauber2, Matthew Cartwright3, Simon Gaines3, Jonathan C Killen3, Olivier René2, Stuart I Ward3, Gladys de Leon Boenig2, Yuzhong Deng2, Céline Eidenschenk2, Christine Everett2, Emanuela Gancia3, Arunima Ganguli3, Alberto Gobbi2, Julie Hawkins3, Adam R Johnson2, James R Kiefer2, Hank La2, Peter Lockey3, Maxine Norman3, Wenjun Ouyang2, Ann Qin2, Nicole Wakes3, Bohdan Waszkowycz3, Harvey Wong2.
Abstract
The identification of a new series of RORc inverse agonists is described. Comprehensive structure-activity relationship studies of this reversed sulfonamide series identified potent RORc inverse agonists in biochemical and cellular assays which were also selective against a panel of nuclear receptors. Our work has contributed a compound that may serve as a useful in vitro tool to delineate the complex biological pathways involved in signalling through RORc. An X-ray co-crystal structure of an analogue with RORc has also provided useful insights into the binding interactions of the new series.Entities:
Keywords: IL-17; Inflammation; RORc; RORγ; RORγt; X-ray structure
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Year: 2014 PMID： 25453817 DOI： 10.1016/j.bmcl.2014.10.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823