Modulators of the Nuclear Receptor Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc)

被引：154

作者：

Fauber, Benjamin P. ^{[1
]}

Magnuson, Steven ^{[1
]}

机构：

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 14期

关键词：

LIGAND-BINDING DOMAIN; COLLAGEN-INDUCED ARTHRITIS; X-RAY-STRUCTURE; CRYSTAL-STRUCTURE; T(H)17 CELLS; TH17; CELLS; CIRCADIAN TRANSCRIPTION; THERAPEUTIC TARGET; STRUCTURAL BASIS; POTENT;

D O I：

10.1021/jm401901d

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

As the biology surrounding the nuclear receptor retinoic acid receptor-related orphan receptor-gamma (ROR gamma or RORc) continues to evolve, significant effort has been invested in discovering modulators of this potentially important target for the treatment of metabolic and immunological diseases. Several major pharmaceutical and biotechnology companies have disclosed RORc inhibitors or partnered with other players in the field. In this perspective, we discuss both the biology and the underlying structural biology of RORc, and summarize the RORc modulators disclosed in the scientific and patent literature.

引用

页码：5871 / 5892

页数：22

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