2rbe

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{{STRUCTURE_2rbe| PDB=2rbe | SCENE= }}
{{STRUCTURE_2rbe| PDB=2rbe | SCENE= }}
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'''The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors'''
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===The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors===
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==Overview==
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A series of 2-anilinothiazolones were prepared as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The most potent compounds contained a 2-chloro or 2-fluoro group on the aniline ring with an isopropyl substituent on the 5-position of the thiazolone ring (compounds 2 and 3, respectively). The binding mode was determined through the X-ray co-crystal structure of the enzyme with compound 3. This compound was also approximately 70-fold selective over 11beta-HSD2 and was orally bioavailable in rat pharmacokinetic studies. However, compound 3 was &gt;580-fold less active in the 11beta-HSD1 cell assay when tested in the presence of 3% human serum albumin.
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(as it appears on PubMed at http://www.pubmed.gov), where 17919905 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17919905}}
==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 Sun May 4 16:36:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:31:49 2008''

Revision as of 11:31, 29 July 2008

Image:2rbe.png

Template:STRUCTURE 2rbe

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors

Template:ABSTRACT PUBMED 17919905

About this Structure

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

Reference

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors., Yuan C, St Jean DJ Jr, Liu Q, Cai L, Li A, Han N, Moniz G, Askew B, Hungate RW, Johansson L, Tedenborg L, Pyring D, Williams M, Hale C, Chen M, Cupples R, Zhang J, Jordan S, Bartberger MD, Sun Y, Emery M, Wang M, Fotsch C, Bioorg Med Chem Lett. 2007 Nov 15;17(22):6056-61. Epub 2007 Sep 25. PMID:17919905

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