1osv

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[[Image:1osv.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_1osv| PDB=1osv | SCENE= }}
{{STRUCTURE_1osv| PDB=1osv | SCENE= }}
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'''STRUCTURAL BASIS FOR BILE ACID BINDING AND ACTIVATION OF THE NUCLEAR RECEPTOR FXR'''
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===STRUCTURAL BASIS FOR BILE ACID BINDING AND ACTIVATION OF THE NUCLEAR RECEPTOR FXR===
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==Overview==
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The nuclear receptor FXR is the sensor of physiological levels of enterohepatic bile acids, the end products of cholesterol catabolism. Here we report crystal structures of the FXR ligand binding domain in complex with coactivator peptide and two different bile acids. An unusual A/B ring juncture, a feature associated with bile acids and no other steroids, provides ligand discrimination and triggers a pi-cation switch that activates FXR. Helix 12, the activation function 2 of the receptor, adopts the agonist conformation and stabilizes coactivator peptide binding. FXR is able to interact simultaneously with two coactivator motifs, providing a mechanism for enhanced binding of coactivators through intermolecular contacts between their LXXLL sequences. These FXR complexes provide direct insights into the design of therapeutic bile acids for treatment of hyperlipidemia and cholestasis.
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(as it appears on PubMed at http://www.pubmed.gov), where 12718893 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12718893}}
==About this Structure==
==About this Structure==
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[[Category: Lbd]]
[[Category: Lbd]]
[[Category: Nuclear receptor]]
[[Category: Nuclear receptor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:14:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:47:15 2008''

Revision as of 00:47, 28 July 2008

Image:1osv.png

Template:STRUCTURE 1osv

STRUCTURAL BASIS FOR BILE ACID BINDING AND ACTIVATION OF THE NUCLEAR RECEPTOR FXR

Template:ABSTRACT PUBMED 12718893

About this Structure

1OSV is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Structural basis for bile acid binding and activation of the nuclear receptor FXR., Mi LZ, Devarakonda S, Harp JM, Han Q, Pellicciari R, Willson TM, Khorasanizadeh S, Rastinejad F, Mol Cell. 2003 Apr;11(4):1093-100. PMID:12718893

Page seeded by OCA on Mon Jul 28 03:47:15 2008

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