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RORγ Structural Plasticity and Druggability

Department of Biochemistry and Molecular Biophysics, Kansas State University, Manhattan, KS 66506, USA
Division of Biology, Kansas State University, Manhattan, KS 66506, USA
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(15), 5329;
Received: 12 June 2020 / Revised: 8 July 2020 / Accepted: 15 July 2020 / Published: 27 July 2020
(This article belongs to the Special Issue Molecular Biology of Nuclear Receptors 2.0)
Retinoic acid receptor-related orphan receptor γ (RORγ) is a transcription factor regulating the expression of the pro-inflammatory cytokine IL-17 in human T helper 17 (Th17) cells. Activating RORγ can induce multiple IL-17-mediated autoimmune diseases but may also be useful for anticancer therapy. Its deep immunological functions make RORɣ an attractive drug target. Over 100 crystal structures have been published describing atomic interactions between RORɣ and agonists and inverse agonists. In this review, we focus on the role of dynamic properties and plasticity of the RORɣ orthosteric and allosteric binding sites by examining structural information from crystal structures and simulated models. We discuss the possible influences of allosteric ligands on the orthosteric binding site. We find that high structural plasticity favors the druggability of RORɣ, especially for allosteric ligands. View Full-Text
Keywords: RORγ; plasticity; druggability; orthosteric binding pocket; allosteric binding pocket RORγ; plasticity; druggability; orthosteric binding pocket; allosteric binding pocket
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MDPI and ACS Style

Huang, M.; Bolin, S.; Miller, H.; Ng, H.L. RORγ Structural Plasticity and Druggability. Int. J. Mol. Sci. 2020, 21, 5329.

AMA Style

Huang M, Bolin S, Miller H, Ng HL. RORγ Structural Plasticity and Druggability. International Journal of Molecular Sciences. 2020; 21(15):5329.

Chicago/Turabian Style

Huang, Mian, Shelby Bolin, Hannah Miller, and Ho Leung Ng. 2020. "RORγ Structural Plasticity and Druggability" International Journal of Molecular Sciences 21, no. 15: 5329.

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