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Article

International Union of Pharmacology. LXIII. Retinoid X Receptors

Institut de Génétique et de Biologie Moléculaire et Cellulaire, 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 (P.G., P.C., H.G.); Max-Planck-Institute of Experimental Endocrinology, Hannover, Germany (G.E.); Howard Hughes Medical Institute, Gene Expression Laboratory, Salk Institute for Biological Studies, La Jolla, California (R.M.E.); Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, and the Institute for Diabetes, Obesity, and Metabolism, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania (M.A.L.); Program in Molecular and Cellular Biology, Oregon State University, Corvallis, Oregon (M.L.); Departamento de Quimica Organica, Facultade de Quimica, Universidade de Vigo, Lagoas Marcosende, Vigo, Galicia, Spain (A.R.d.L.); Department of Thoracic/Head and Neck Medical Oncology-Unit 432, The University of Texas MD Anderson Cancer Center, Houston, Texas (R.L.); and Howard Hughes Medical Institute, Department of Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas (D.J.M.)

Abstract

Introduction

The RXRs

Ligands

Expression and Function of RXRs

Therapy and Diseases

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, RXR, RXR, and RXR. 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.

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International Union of Pharmacology. LX. Retinoic Acid Receptors

Pierre Germain, Pierre Chambon, Gregor Eichele, Ronald M. Evans, Mitchell A. Lazar, Mark Leid, Angel R. De Lera, Reuben Lotan, David J. Mangelsdorf, and Hinrich Gronemeyer
Pharmacological Reviews 2006 58: 712-725. [Abstract] [Full Text]  

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