2ihq

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[[Image:2ihq.jpg|left|200px]]
[[Image:2ihq.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2ihq |SIZE=350|CAPTION= <scene name='initialview01'>2ihq</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2ihq", 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=LG7:4-[(7R,7AS)-7-HYDROXY-1,3-DIOXOTETRAHYDRO-1H-PYRROLO[1,2-C]IMIDAZOL-2(3H)-YL]-1-NAPHTHONITRILE'>LG7</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= Ar ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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-->
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|DOMAIN=
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{{STRUCTURE_2ihq| PDB=2ihq | SCENE= }}
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|RELATEDENTRY=[[1i37|1I37]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ihq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ihq OCA], [http://www.ebi.ac.uk/pdbsum/2ihq PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ihq RCSB]</span>
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}}
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'''Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin'''
'''Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Sack, J S.]]
[[Category: Sack, J S.]]
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[[Category: androgen receptor]]
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[[Category: Androgen receptor]]
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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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[[Category: steroid receptor]]
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[[Category: Steroid receptor]]
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[[Category: transcription regulation]]
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[[Category: Transcription regulation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:31:03 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:44:34 2008''
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Revision as of 04:31, 4 May 2008

Image:2ihq.jpg

Template:STRUCTURE 2ihq

Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin


Overview

A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited >50-fold selectivity for muscle over prostate.

About this Structure

2IHQ is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold., Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG, J Med Chem. 2006 Dec 28;49(26):7596-9. PMID:17181141 Page seeded by OCA on Sun May 4 07:31:03 2008

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OCA

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