International Union of Pharmacology. LXIII. Retinoid X receptors.
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, RXRalpha, RXRbeta, and RXRgamma. 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.
Germain
Pierre
P
Centre National de la Recherche Scientifique/Institut National de la Santé et de la Recherche Médicale/Université Louis Pasteur, Illkirch, Communauté Urbaine de Strasbourg, France. germain@titus.u-strasbg.fr
Chambon
Pierre
P
Eichele
Gregor
G
Evans
Ronald M
RM
Lazar
Mitchell A
MA
Leid
Mark
M
De Lera
Angel R
AR
Lotan
Reuben
R
Mangelsdorf
David J
DJ
Gronemeyer
Hinrich
H
D000818:Animals; D015870:Gene Expression; D006801:Humans; D008024:Ligands; D009154:Mutation; D047488:Retinoid X Receptors / Q000145:classification / Q000235:genetics / Q000502:physiology*; D012176:Retinoids / Q000502:physiology*; D009626:Terminology as Topic
D008024:Ligands; D047488:Retinoid X Receptors; D012176:Retinoids