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3cwe

From Proteopedia

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[[Image:3cwe.jpg|left|200px]]
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{{STRUCTURE_3cwe| PDB=3cwe | SCENE= }}
{{STRUCTURE_3cwe| PDB=3cwe | SCENE= }}
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'''PTP1B in complex with a phosphonic acid inhibitor'''
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===PTP1B in complex with a phosphonic acid inhibitor===
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==Overview==
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A series of quinoline/naphthalene-difluoromethylphosphonates were prepared and were found to be potent PTP1B inhibitors. Most of these compounds bearing polar functionalities or large lipophilic residues did not show appreciable oral bioavailability in rodents while small and less polar analogs displayed moderate to good oral bioavailability. The title compound was found to have the best overall potency and pharmacokinetic profile and was found to be efficacious in animal models of diabetes and cancer.
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{{ABSTRACT_PUBMED_18477508}}
==About this Structure==
==About this Structure==
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[[Category: Polymorphism]]
[[Category: Polymorphism]]
[[Category: Protein phosphatase]]
[[Category: Protein phosphatase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 11 10:50:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 11:28:10 2008''

Revision as of 08:28, 29 July 2008

Image:3cwe.png

Template:STRUCTURE 3cwe

PTP1B in complex with a phosphonic acid inhibitor

Template:ABSTRACT PUBMED 18477508

About this Structure

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

Reference

Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor., Han Y, Belley M, Bayly CI, Colucci J, Dufresne C, Giroux A, Lau CK, Leblanc Y, McKay D, Therien M, Wilson MC, Skorey K, Chan CC, Scapin G, Kennedy BP, Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5. Epub 2008 Apr 29. PMID:18477508

Page seeded by OCA on Tue Jul 29 11:28:10 2008

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