1osh

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[[Image:1osh.jpg|left|200px]]
[[Image:1osh.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1osh |SIZE=350|CAPTION= <scene name='initialview01'>1osh</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_1osh", 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=FEX:METHYL+3-{3-[(CYCLOHEXYLCARBONYL){[4&#39;-(DIMETHYLAMINO)BIPHENYL-4-YL]METHYL}AMINO]PHENYL}ACRYLATE'>FEX</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= NR1H4 ([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_1osh| PDB=1osh | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1osh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1osh OCA], [http://www.ebi.ac.uk/pdbsum/1osh PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1osh RCSB]</span>
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'''A Chemical, Genetic, and Structural Analysis of the nuclear bile acid receptor FXR'''
'''A Chemical, Genetic, and Structural Analysis of the nuclear bile acid receptor FXR'''
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[[Category: Rosenfeld, J M.]]
[[Category: Rosenfeld, J M.]]
[[Category: Verdecia, M A.]]
[[Category: Verdecia, M A.]]
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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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:13:49 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:49:43 2008''
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Revision as of 01:13, 3 May 2008

Image:1osh.jpg

Template:STRUCTURE 1osh

A Chemical, Genetic, and Structural Analysis of the nuclear bile acid receptor FXR


Overview

The farnesoid X receptor (FXR) functions as a bile acid (BA) sensor coordinating cholesterol metabolism, lipid homeostasis, and absorption of dietary fats and vitamins. However, BAs are poor reagents for characterizing FXR functions due to multiple receptor independent properties. Accordingly, using combinatorial chemistry we evolved a small molecule agonist termed fexaramine with 100-fold increased affinity relative to natural compounds. Gene-profiling experiments conducted in hepatocytes with FXR-specific fexaramine versus the primary BA chenodeoxycholic acid (CDCA) produced remarkably distinct genomic targets. Highly diffracting cocrystals (1.78 A) of fexaramine bound to the ligand binding domain of FXR revealed the agonist sequestered in a 726 A(3) hydrophobic cavity and suggest a mechanistic basis for the initial step in the BA signaling pathway. The discovery of fexaramine will allow us to unravel the FXR genetic network from the BA network and selectively manipulate components of the cholesterol pathway that may be useful in treating cholesterol-related human diseases.

About this Structure

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

Reference

A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR., Downes M, Verdecia MA, Roecker AJ, Hughes R, Hogenesch JB, Kast-Woelbern HR, Bowman ME, Ferrer JL, Anisfeld AM, Edwards PA, Rosenfeld JM, Alvarez JG, Noel JP, Nicolaou KC, Evans RM, Mol Cell. 2003 Apr;11(4):1079-92. PMID:12718892 Page seeded by OCA on Sat May 3 04:13:49 2008

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