2ihq

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{{STRUCTURE_2ihq| PDB=2ihq | SCENE= }}
{{STRUCTURE_2ihq| PDB=2ihq | SCENE= }}
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'''Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin'''
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===Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin===
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==Overview==
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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 &gt;50-fold selectivity for muscle over prostate.
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(as it appears on PubMed at http://www.pubmed.gov), where 17181141 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17181141}}
==About this Structure==
==About this Structure==
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[[Category: Steroid receptor]]
[[Category: Steroid receptor]]
[[Category: Transcription regulation]]
[[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 Tue Jul 29 00:02:30 2008''

Revision as of 21:02, 28 July 2008

Image:2ihq.png

Template:STRUCTURE 2ihq

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

Template:ABSTRACT PUBMED 17181141

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

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