1fby
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(New page: 200px<br /> <applet load="1fby" size="450" color="white" frame="true" align="right" spinBox="true" caption="1fby, resolution 2.25Å" /> '''CRYSTAL STRUCTURE O...)
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Revision as of 14:44, 12 November 2007
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CRYSTAL STRUCTURE OF THE HUMAN RXR ALPHA LIGAND BINDING DOMAIN BOUND TO 9-CIS RETINOIC ACID
Overview
The pleiotropic effects of active retinoids are transduced by their, cognate nuclear receptors, retinoid X receptors (RXRs) and retinoic acid, receptors (RARs), which act as transcriptional regulators activated by two, stereoisomers of retinoic acid (RA): 9-cis RA (9-cRA) and all-trans RA, (a-tRA). Among nuclear receptors, RXR occupies a central position and, plays a crucial role in many intracellular signalling pathways as a, ubiquitous heterodimerization partner with numerous other members of this, superfamily. Whereas RARs bind both isomers, RXRs exclusively bind 9-cRA., The crystal structure of the ligand-binding domain (LBD) of human RXRalpha, bound to 9-cRA reveals the molecular basis of this ligand selectivity and, allows a comparison of both apo and holo forms of the same nuclear, receptor. In the crystal, the receptor is monomeric and exhibits a, canonical agonist conformation without direct contacts between the ligand, and the transactivation helix H12. Comparison with the unliganded RXRalpha, LBD structure reveals the molecular mechanisms of ligand-induced, conformational changes and allows us to describe at the atomic level how, these changes generate the proper protein interface involved in nuclear, receptor-coactivator interaction.
About this Structure
1FBY is a Single protein structure of sequence from Homo sapiens with REA as ligand. Full crystallographic information is available from OCA.
Reference
Crystal structure of the human RXRalpha ligand-binding domain bound to its natural ligand: 9-cis retinoic acid., Egea PF, Mitschler A, Rochel N, Ruff M, Chambon P, Moras D, EMBO J. 2000 Jun 1;19(11):2592-601. PMID:10835357
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