RXRα Inhibitors

RXRα inhibitors constitute a class of compounds designed to interfere with the function of the Retinoid X Receptor alpha (RXRα). RXRα belongs to the nuclear receptor superfamily and serves as a crucial transcription factor involved in regulating gene expression by forming heterodimers with various partners, including other nuclear receptors like peroxisome proliferator-activated receptor (PPAR), liver X receptor (LXR), and retinoic acid receptor (RAR). These heterodimers play pivotal roles in modulating gene transcription by binding to specific DNA sequences known as response elements within the promoter regions of target genes. RXRα, as a common partner in these heterodimers, functions as a critical mediator in diverse signaling pathways, influencing various biological processes such as cell differentiation, proliferation, metabolism, and immune response.

Inhibitors targeting RXRα interfere with its activity by disrupting the formation or function of RXRα-containing heterodimers. These inhibitors often act by binding to RXRα or its partner proteins, thereby preventing the assembly of functional transcription complexes or impeding their ability to bind to specific DNA sequences.