Modulation of RXR function through ligand design

► RXRs are promiscuous partners in heterodimers with other nuclear receptors. ► Permissive heterodimers are responsive to ligands of each partner. ► Ligand structure is linked to cofactor interactions and physiological function. ► Rexinoids are promising drugs for the treatment of the Metabolic Syndrome. ► RXR/PPARγ and RXR/LXR heterodimer-specific rexinoids have been developed.