4.7 Article

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 24, Pages 10976-10995

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b00588

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The nuclear receptor retinoic acid receptor-related orphan receptor gamma (ROR gamma 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.

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