1xap

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[[Image:1xap.jpg|left|200px]]
[[Image:1xap.jpg|left|200px]]
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{{Structure
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|PDB= 1xap |SIZE=350|CAPTION= <scene name='initialview01'>1xap</scene>, resolution 2.1&Aring;
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The line below this paragraph, containing "STRUCTURE_1xap", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=TTB:4-[(1E)-2-(5,5,8,8-TETRAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PROP-1-ENYL]BENZOIC+ACID'>TTB</scene>
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{{STRUCTURE_1xap| PDB=1xap | SCENE= }}
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1xap FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xap OCA], [http://www.ebi.ac.uk/pdbsum/1xap PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1xap RCSB]</span>
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'''Structure of the ligand binding domain of the Retinoic Acid Receptor beta'''
'''Structure of the ligand binding domain of the Retinoic Acid Receptor beta'''
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[[Category: Tortolani, D.]]
[[Category: Tortolani, D.]]
[[Category: Zusi, F C.]]
[[Category: Zusi, F C.]]
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[[Category: ligand binding domain]]
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[[Category: Ligand binding domain]]
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[[Category: nuclear receptor]]
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[[Category: Nuclear receptor]]
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[[Category: retinoic acid receptor beta]]
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[[Category: Retinoic acid receptor beta]]
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[[Category: ttnpb]]
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[[Category: Ttnpb]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:47:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:47:06 2008''
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Revision as of 11:47, 3 May 2008

Image:1xap.jpg

Template:STRUCTURE 1xap

Structure of the ligand binding domain of the Retinoic Acid Receptor beta


Overview

The crystal structure of the ligand-binding domain of RARbeta, a suspect tumour suppressor, reveals important features that distinguish it from the two other RAR isotypes. The most striking difference is an extra cavity allowing RARbeta to bind more bulky agonists. Accordingly, we identified a ligand that shows RARbeta selectivity with a 100-fold higher affinity to RARbeta than to alpha or gamma isotypes. The structural differences between the three RAR ligand-binding pockets revealed a rationale explaining how a single retinoid can be at the same time an RARalpha, gamma antagonist and an RARbeta agonist. In addition, we demonstrate how to generate an RARbeta antagonist by gradually modifying the bulkiness of a single substitution. Together, our results provide structural guidelines for the synthesis of RARbeta-selective agonists and antagonists, allowing for the first time to address pharmacologically the tumour suppressor role of RARbeta in vitro and in animal models.

About this Structure

1XAP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Rational design of RAR-selective ligands revealed by RARbeta crystal stucture., Germain P, Kammerer S, Perez E, Peluso-Iltis C, Tortolani D, Zusi FC, Starrett J, Lapointe P, Daris JP, Marinier A, de Lera AR, Rochel N, Gronemeyer H, EMBO Rep. 2004 Sep;5(9):877-82. PMID:15319780 Page seeded by OCA on Sat May 3 14:47:29 2008

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