3czr

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{{STRUCTURE_3czr| PDB=3czr | SCENE= }}
{{STRUCTURE_3czr| PDB=3czr | SCENE= }}
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'''Crystal Structure of Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) in Complex with Arylsulfonylpiperazine Inhibitor'''
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===Crystal Structure of Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) in Complex with Arylsulfonylpiperazine Inhibitor===
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==Overview==
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High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11beta-Hydroxysteroid Dehydrogenase Type 1 (11beta-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11beta-HSD1 IC(50)=3nM).
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{{ABSTRACT_PUBMED_18511278}}
==About this Structure==
==About this Structure==
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[[Category: Steroid metabolism]]
[[Category: Steroid metabolism]]
[[Category: Transmembrane]]
[[Category: Transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 18 12:12:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:53:08 2008''

Revision as of 14:53, 27 July 2008

Image:3czr.png

Template:STRUCTURE 3czr

Crystal Structure of Human 11-beta-Hydroxysteroid Dehydrogenase (HSD1) in Complex with Arylsulfonylpiperazine Inhibitor

Template:ABSTRACT PUBMED 18511278

About this Structure

3CZR is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)., Sun D, Wang Z, Di Y, Jaen JC, Labelle M, Ma J, Miao S, Sudom A, Tang L, Tomooka CS, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP, Bioorg Med Chem Lett. 2008 Jun 15;18(12):3513-6. Epub 2008 May 10. PMID:18511278

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