1pq9

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[[Image:1pq9.gif|left|200px]]
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{{Seed}}
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[[Image:1pq9.png|left|200px]]
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{{STRUCTURE_1pq9| PDB=1pq9 | SCENE= }}
{{STRUCTURE_1pq9| PDB=1pq9 | SCENE= }}
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'''HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 COMPLEX'''
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===HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 COMPLEX===
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==Overview==
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The structures of the liver X receptor LXRbeta (NR1H2) have been determined in complexes with two synthetic ligands, T0901317 and GW3965, to 2.1 and 2.4 A, respectively. Together with its isoform LXRalpha (NR1H3) it regulates target genes involved in metabolism and transport of cholesterol and fatty acids. The two LXRbeta structures reveal a flexible ligand-binding pocket that can adjust to accommodate fundamentally different ligands. The ligand-binding pocket is hydrophobic but with polar or charged residues at the two ends of the cavity. T0901317 takes advantage of this by binding to His-435 close to H12 while GW3965 orients itself with its charged group in the opposite direction. Both ligands induce a fixed "agonist conformation" of helix H12 (also called the AF-2 domain), resulting in a transcriptionally active receptor.
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The line below this paragraph, {{ABSTRACT_PUBMED_12819202}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 12819202 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12819202}}
==About this Structure==
==About this Structure==
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[[Category: Wilhelmsson, A.]]
[[Category: Wilhelmsson, A.]]
[[Category: Lxrb+t0901317 split]]
[[Category: Lxrb+t0901317 split]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:21:50 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 20:38:18 2008''

Revision as of 17:38, 27 July 2008

Image:1pq9.png

Template:STRUCTURE 1pq9

HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 COMPLEX

Template:ABSTRACT PUBMED 12819202

About this Structure

1PQ9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands., Farnegardh M, Bonn T, Sun S, Ljunggren J, Ahola H, Wilhelmsson A, Gustafsson JA, Carlquist M, J Biol Chem. 2003 Oct 3;278(40):38821-8. Epub 2003 Jun 20. PMID:12819202

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