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J Med Chem. 2014 Jul 24;57(14):5871-92. doi: 10.1021/jm401901d. Epub 2014 Feb 24.

Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).

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Discovery Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.


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.

[Indexed for MEDLINE]

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