1dkf: Difference between revisions

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|PDB= 1dkf |SIZE=350|CAPTION= <scene name='initialview01'>1dkf</scene>, resolution 2.50&Aring;
|PDB= 1dkf |SIZE=350|CAPTION= <scene name='initialview01'>1dkf</scene>, resolution 2.50&Aring;
|SITE=  
|SITE=  
|LIGAND= <scene name='pdbligand=BMS:4-[(4,4-DIMETHYL-1,2,3,4-TETRAHYDRO-[1,2']BINAPTHALENYL-7-CARBONYL)-AMINO]-BENZOIC+ACID'>BMS</scene> and <scene name='pdbligand=OLA:OLEIC ACID'>OLA</scene>
|LIGAND= <scene name='pdbligand=BMS:4-[(4,4-DIMETHYL-1,2,3,4-TETRAHYDRO-[1,2&#39;]BINAPTHALENYL-7-CARBONYL)-AMINO]-BENZOIC+ACID'>BMS</scene> and <scene name='pdbligand=OLA:OLEIC ACID'>OLA</scene>
|ACTIVITY=  
|ACTIVITY=  
|GENE=  
|GENE=  
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[[Category: structural proteomics in europe]]
[[Category: structural proteomics in europe]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 10:39:49 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 23 11:31:28 2008''

Revision as of 09:31, 23 March 2008

File:1dkf.gif


Drag the structure with the mouse to rotate
1dkf, resolution 2.50Å
Ligands: BMS and OLA
Coordinates: save as pdb, mmCIF, xml



CRYSTAL STRUCTURE OF A HETERODIMERIC COMPLEX OF RAR AND RXR LIGAND-BINDING DOMAINS


Overview

The crystal structure of a heterodimer between the ligand-binding domains (LBDs) of the human RARalpha bound to a selective antagonist and the constitutively active mouse RXRalphaF318A mutant shows that, pushed by a bulky extension of the ligand, RARalpha helix H12 adopts an antagonist position. The unexpected presence of a fatty acid in the ligand-binding pocket of RXRalpha(F318A is likely to account for its apparent "constitutivity." Specific conformational changes suggest the structural basis of pure and partial antagonism. The RAR-RXR heterodimer interface is similar to that observed in most nuclear receptor (NR) homodimers. A correlative analysis of 3D structures and sequences provides a novel view on dimerization among members of the nuclear receptor superfamily.

Disease

Known disease associated with this structure: Leukemia, acute promyelocytic OMIM:[180240]

About this Structure

1DKF is a Protein complex structure of sequences from Homo sapiens and Mus musculus. Full crystallographic information is available from OCA.

Reference

Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains., Bourguet W, Vivat V, Wurtz JM, Chambon P, Gronemeyer H, Moras D, Mol Cell. 2000 Feb;5(2):289-98. PMID:10882070

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