Retinoid receptor ligand-binding domain

The ligand-binding domain (LBD) of retinoid receptors (RARs and RXRs) is a highly conserved region that binds endogenous retinoids (vitamin A derivatives) and synthetic ligands. Ligand binding promotes conformational changes resulting in activation or repression of target gene transcription. The LBD also mediates receptor dimerization, recruitment of coactivators/corepressors, and allosteric communication with the DNA-binding domain. Retinoid receptors regulate fundamental processes such as embryonic development, differentiation, metabolism, and homeostasis, and play roles in development, cancer, and other diseases. Drugs targeting the LBD are clinically important for treating leukemia, skin disorders, and metabolic diseases, but safety concerns such as teratogenicity and organ toxicity limit their use.

Other names

Retinoic acid receptor ligand-binding domainRetinoid X receptor ligand-binding domainNuclear receptor ligand-binding domain

Ligand binding induces conformational changes in the receptor, activating transcriptional coactivators and promoting gene expression or repressing by corepressor dissociation; Some drugs act as receptor agonists or antagonists, modulating transcriptional activity