Recent progress on nuclear receptor RORγ modulators

被引：75

作者：

Cyr, Patrick ^{[1
]}

Bronner, Sarah M. ^{[1
]}

Crawford, James J. ^{[1
]}

机构：

[1] Genentech Inc, Discovery Chem, 1 DNA Way, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 18期

关键词：

ROR gamma; RORc; IL-17; T INVERSE AGONISTS; T(H)17 CELLS; STRUCTURAL BASIS; GENE-EXPRESSION; DRUG TARGETS; IN-VIVO; DISCOVERY; POTENT; DIFFERENTIATION; IDENTIFICATION;

D O I：

10.1016/j.bmcl.2016.08.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The retinoic acid receptor-related orphan receptor ROR gamma plays key roles in the development and differentiation of T(H)17 cells, and thus in IL-17 expression, thymocyte development and regulation of metabolism. With the recent progression into phase 2 clinical trials of both oral and topically administered inverse agonists, and with others close behind, there is significant interest in the discovery of ROR gamma modulators. This digest covers key developments around ROR gamma agonists, antagonists and inverse agonists; orthosteric and allosteric binders; and aims to summarize the available information concerning the potential utility of ROR gamma modulators. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：4387 / 4393

页数：7

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