Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses,Journal of Medicinal Chemistry

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Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2018-07-16 00:00:00 , DOI: 10.1021/acs.jmedchem.8b00588
Vrajesh B. Pandya ₁ , Sanjay Kumar ₁ , Sachchidanand ₁ , Rajiv Sharma ₁ , Ranjit C. Desai ₁

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The nuclear receptor retinoic acid receptor-related orphan receptor gamma (RORγ or RORc) is a key transcription factor for the production of pro-inflammatory cytokines implicated in the pathogenesis of autoimmune diseases. Recently, small molecule inhibitors of RORc drew the enormous attention of the research community worldwide as a possible therapy for autoimmune diseases, mediated by the IL-17 cytokine. With the clinical proof-of-concept inferred from a small molecule inhibitor VTP-43742 for psoriasis and recent inflow of several RORc inhibitors into the clinic for therapeutic interventions in autoimmune diseases, this field continues to evolve. This review briefly summarizes the RORc inhibitors disclosed in the literature and discusses the progress made by these inhibitors in combating autoimmune diseases.

中文翻译：

与视黄酸受体相关的孤儿受体-γ（RORγ或RORc）抑制剂对抗自身免疫性疾病：命中注定

核受体视黄酸受体相关的孤儿受体γ（RORγ或RORc）是产生与自身免疫性疾病发病机制有关的促炎性细胞因子的关键转录因子。最近，RORc的小分子抑制剂作为IL-17细胞因子介导的自身免疫性疾病的一种可能疗法引起了全世界研究界的极大关注。从用于牛皮癣的小分子抑制剂VTP-43742推断出的临床概念证明，以及最近几种RORc抑制剂进入临床以治疗自身免疫性疾病的临床干预措施，该领域仍在不断发展。这篇综述简要总结了文献中公开的RORc抑制剂，并讨论了这些抑制剂在对抗自身免疫性疾病方面取得的进展。

更新日期：2018-07-16

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