1pqc

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[[Image:1pqc.gif|left|200px]]
[[Image:1pqc.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1pqc |SIZE=350|CAPTION= <scene name='initialview01'>1pqc</scene>, resolution 2.80&Aring;
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The line below this paragraph, containing "STRUCTURE_1pqc", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=444:N-(2,2,2-TRIFLUOROETHYL)-N-{4-[2,2,2-TRIFLUORO-1-HYDROXY-1-(TRIFLUOROMETHYL)ETHYL]PHENYL}BENZENESULFONAMIDE'>444</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= NR1H2 OR LXRB OR UNR OR NER ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1pqc| PDB=1pqc | SCENE= }}
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|RELATEDENTRY=[[1pq9|1pq9]], [[1pq6|1pq6]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1pqc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pqc OCA], [http://www.ebi.ac.uk/pdbsum/1pqc PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1pqc RCSB]</span>
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}}
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'''HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317'''
'''HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317'''
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[[Category: Sun, S.]]
[[Category: Sun, S.]]
[[Category: Wilhelmsson, A.]]
[[Category: Wilhelmsson, A.]]
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[[Category: lxrb+t0901317]]
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[[Category: Lxrb+t0901317]]
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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 Mar 30 23:03:07 2008''
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Revision as of 02:21, 3 May 2008

Image:1pqc.gif

Template:STRUCTURE 1pqc

HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317


Overview

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.

About this Structure

1PQC 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 Page seeded by OCA on Sat May 3 05:21:50 2008

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