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

Modulators of the Nuclear Receptor Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc)
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DOI:
10.1021/jm401901d
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发表时间:
2014-07-24
影响因子:
7.3
通讯作者:
Magnuson, Steven
Magnuson, Steven
中科院分区:
医学1区
文献类型:
--
作者:
Fauber, Benjamin P.;Magnuson, Steven

文献摘要

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随着围绕核受体视黄酸受体相关孤儿受体-γ(ROR γ或RORc)的生物学的持续发展,已经投入大量努力来发现用于治疗代谢和免疫疾病的这种潜在重要靶标的调节剂。几家主要的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。从这个角度来看,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公开的RORc调节剂。
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.