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Recent Progress in the Design and Discovery of RXR Modulators Targeting Alternate Binding Sites of the Receptor

[ Vol. 17 , Issue. 6 ]

Author(s):

Ying Su, Zhiping Zeng, Ziwen Chen, Dan Xu, Weidong Zhang and Xiao-kun Zhang   Pages 663 - 675 ( 13 )

Abstract:


Retinoid X receptors (RXRs) occupy a central position within the nuclear receptor superfamily. They not only function as important transcriptional factors but also exhibit diverse nongenomic biological activities. The pleiotropic actions of RXRs under both physiological and pathophysiological conditions confer RXRs important drug targets for the treatment of cancer, and metabolic and neurodegenerative diseases. RXR modulators have been studied for the purpose of developing both drug molecules and chemical tools for biological investigation of RXR. Development of RXR modulators has focused on small molecules targeting the canonical ligand-binding pocket. However, accumulating results have demonstrated that there are other binding mechanisms by which small molecules interact with RXR to act as RXR modulators. This review discusses the recent development in the design and discovery of RXR modulators with a focus on those targeting novel binding sites on RXR.

Keywords:

RXRα, tRXRα, Rexinoid, RXRα modulators, Nongenomic action, Nuclear receptors, NSAID, Apoptosis, Inflammation, PI3K

Affiliation:

Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Road, La Jolla, California 92037,, School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102

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