1ilh

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:1ilh.gif|left|200px]]
[[Image:1ilh.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 1ilh |SIZE=350|CAPTION= <scene name='initialview01'>1ilh</scene>, resolution 2.76&Aring;
+
The line below this paragraph, containing "STRUCTURE_1ilh", creates the "Structure Box" on the page.
-
|SITE=
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=SRL:[2-(3,5-DI-TERT-BUTYL-4-HYDROXY-PHENYL)-1-(DIETHOXY-PHOSPHORYL)-VINYL]-PHOSPHONIC+ACID+DIETHLYL+ESTER'>SRL</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY=
+
or leave the SCENE parameter empty for the default display.
-
|GENE= PXR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+
-->
-
|DOMAIN=
+
{{STRUCTURE_1ilh| PDB=1ilh | SCENE= }}
-
|RELATEDENTRY=[[1ilg|1ILG]]
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ilh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ilh OCA], [http://www.ebi.ac.uk/pdbsum/1ilh PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ilh RCSB]</span>
+
-
}}
+
'''Crystal Structure of Human Pregnane X Receptor Ligand Binding Domain Bound to SR12813'''
'''Crystal Structure of Human Pregnane X Receptor Ligand Binding Domain Bound to SR12813'''
Line 27: Line 24:
[[Category: Redinbo, M R.]]
[[Category: Redinbo, M R.]]
[[Category: Watkins, R E.]]
[[Category: Watkins, R E.]]
-
[[Category: ligand]]
+
[[Category: Ligand]]
-
[[Category: multiple binding mode]]
+
[[Category: Multiple binding mode]]
-
[[Category: nuclear receptor]]
+
[[Category: Nuclear receptor]]
-
[[Category: promiscuous]]
+
[[Category: Promiscuous]]
-
[[Category: xenobiotic]]
+
[[Category: Xenobiotic]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 20:07:51 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:21:27 2008''
+

Revision as of 17:07, 2 May 2008

Image:1ilh.gif

Template:STRUCTURE 1ilh

Crystal Structure of Human Pregnane X Receptor Ligand Binding Domain Bound to SR12813


Overview

The human nuclear pregnane X receptor (hPXR) activates cytochrome P450-3A expression in response to a wide variety of xenobiotics and plays a critical role in mediating dangerous drug-drug interactions. We present the crystal structures of the ligand-binding domain of hPXR both alone and in complex with the cholesterol-lowering drug SR12813 at resolutions of 2.5 and 2.75 angstroms, respectively. The hydrophobic ligand-binding cavity of hPXR contains a small number of polar residues, permitting SR12813 to bind in three distinct orientations. The position and nature of these polar residues were found to be critical for establishing the precise pharmacologic activation profile of PXR. Our findings provide important insights into how hPXR detects xenobiotics and may prove useful in predicting and avoiding drug-drug interactions.

About this Structure

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

Reference

The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity., Watkins RE, Wisely GB, Moore LB, Collins JL, Lambert MH, Williams SP, Willson TM, Kliewer SA, Redinbo MR, Science. 2001 Jun 22;292(5525):2329-33. Epub 2001 Jun 14. PMID:11408620 Page seeded by OCA on Fri May 2 20:07:51 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1ilh"
Personal tools