RT Journal Article
SR Electronic
T1 International Union of Pharmacology. LXIII. Retinoid X Receptors
JF Pharmacological Reviews
JO Pharmacol Rev
FD American Society for Pharmacology and Experimental Therapeutics
SP 760
OP 772
DO 10.1124/pr.58.4.7
VO 58
IS 4
A1 Germain, Pierre
A1 Chambon, Pierre
A1 Eichele, Gregor
A1 Evans, Ronald M.
A1 Lazar, Mitchell A.
A1 Leid, Mark
A1 De Lera, Angel R.
A1 Lotan, Reuben
A1 Mangelsdorf, David J.
A1 Gronemeyer, Hinrich
YR 2006
UL http://pharmrev.aspetjournals.org/content/58/4/760.abstract
AB The physiological effects of retinoic acids (RAs) are mediated by members of two families of nuclear receptors, the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs), which are encoded by three distinct human genes, RXRα, RXRβ, and RXRγ. RARs bind both all-trans- and 9-cis-RA, whereas only the 9-cis-RA stereoisomer binds to RXRs. As RXR/RAR heterodimers, these receptors control the transcription of RA target genes through binding to RA-response elements. This review is focused on the structure, mode of action, ligands, expression, and pharmacology of RXRs. Given their role as common partners to many other members of the nuclear receptor superfamily, these receptors have been the subject of intense scrutiny. Moreover, and despite numerous studies since their initial discovery, RXRs remain enigmatic nuclear receptors, and there is still no consensus regarding their role. Indeed, multiple questions about the actual biological role of RXRs and the existence of an endogenous ligand have still to be answered.