Discovery Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
J Med Chem. 2014 Jul 24;57(14):5871-92. doi: 10.1021/jm401901d. Epub 2014 Feb 24.
As the biology surrounding the nuclear receptor retinoic acid receptor-related orphan receptor-gamma (RORγ 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.
随着核受体视黄酸受体相关孤儿受体-γ(RORγ或 RORc)相关生物学的不断发展,人们投入了大量精力来发现这种潜在重要靶点的调节剂,以治疗代谢和免疫性疾病。几家大型制药和生物技术公司已经披露了 RORc 抑制剂,或与该领域的其他参与者合作。在这篇观点文章中,我们讨论了 RORc 的生物学和基础结构生物学,并总结了科学和专利文献中披露的 RORc 调节剂。