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,
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