2hvc: Difference between revisions

Revision as of 06:45, 4 May 2008

The Crystal Structure of Ligand-binding Domain (LBD) of human Androgen Receptor in Complex with a selective modulator LGD2226

OverviewOverview

The androgen receptor (AR) is a ligand-inducible steroid hormone receptor that mediates androgen action, determining male sexual phenotypes and promoting spermatogenesis. As the androgens play a dominant role in male sexual development and function, steroidal androgen agonists have been used clinically for some years. However, there is a risk of potential side effects and most steroidal androgens cannot be dosed orally, which limits the use of these substances. 1,2-Dihydro-6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quino linone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective AR modulator. The crystal structure of the complex of LGD2226 with the androgen receptor ligand-binding domain (AR LBD) at 2.1 A was solved and compared with the structure of the AR LBD-R1881 complex. It is hoped that this will aid in further explaining the selectivity of LGD2226 observed in in vitro and in vivo assays and in developing more selective and effective therapeutic agents.

About this StructureAbout this Structure

2HVC is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226., Wang F, Liu XQ, Li H, Liang KN, Miner JN, Hong M, Kallel EA, van Oeveren A, Zhi L, Jiang T, Acta Crystallogr Sect F Struct Biol Cryst Commun. 2006 Nov 1;62(Pt, 11):1067-71. Epub 2006 Oct 25. PMID:17077481 Page seeded by OCA on Sun May 4 06:45:23 2008

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OCA

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 [[Image:2hvc.jpg|left|200px]]
- {{Structure
+<!--
-|PDB= 2hvc |SIZE=350|CAPTION= <scene name='initialview01'>2hvc</scene>, resolution 2.1&Aring;
+The line below this paragraph, containing "STRUCTURE_2hvc", 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=LGD:6-[BIS(2,2,2-TRIFLUOROETHYL)AMINO]-4-(TRIFLUOROMETHYL)QUINOLIN-2(1H)-ONE'>LGD</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= AR, DHTR, NR3C4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+-->
-|DOMAIN=
+{{STRUCTURE_2hvc|  PDB=2hvc  |  SCENE=  }}
-|RELATEDENTRY=
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2hvc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hvc OCA], [http://www.ebi.ac.uk/pdbsum/2hvc PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2hvc RCSB]</span>
-}}
 '''The Crystal Structure of Ligand-binding Domain (LBD) of human Androgen Receptor in Complex with a selective modulator LGD2226'''
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 [[Category: Wang, F.]]
 [[Category: Zhi, L.]]
-[[Category: complexed with lgd2226]]
+[[Category: Complexed with lgd2226]]
-[[Category: dna-binding]]
+[[Category: Dna-binding]]
-[[Category: ligand binding protein]]
+[[Category: Ligand binding protein]]
-[[Category: steroid-binding]]
+[[Category: Steroid-binding]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 06:45:23 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:35:55 2008''