2nta

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{{STRUCTURE_2nta| PDB=2nta | SCENE= }}
{{STRUCTURE_2nta| PDB=2nta | SCENE= }}
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'''Crystal Structure of PTP1B-inhibitor Complex'''
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===Crystal Structure of PTP1B-inhibitor Complex===
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==Overview==
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The following account describes our systematic effort to replace one of the carboxylate groups of our diacid thiophene PTP1B inhibitors. Active hits were validated using enzymatic assays before pursuing efforts to improve the potency. Only when the C2 carboxylic acid was replaced with another ionizable functional group was reversible and competitive inhibition retained. Use of a tetrazole ring or 1,2,5-thiadiazolidine-3-one-1,1-dioxide as a carboxylate mimetic led to the discovery of two unique starting series that showed improved permeability (PAMPA) and potency of the order of 300nM. The SAR from these efforts underscores some of the major challenges in developing small molecule inhibitors for PTP1B.
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(as it appears on PubMed at http://www.pubmed.gov), where 17336064 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17336064}}
==About this Structure==
==About this Structure==
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[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
[[Category: Ptp1b]]
[[Category: Ptp1b]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:06:40 2008''

Revision as of 04:06, 29 July 2008

Image:2nta.png

Template:STRUCTURE 2nta

Crystal Structure of PTP1B-inhibitor Complex

Template:ABSTRACT PUBMED 17336064

About this Structure

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

Reference

Probing acid replacements of thiophene PTP1B inhibitors., Wan ZK, Follows B, Kirincich S, Wilson D, Binnun E, Xu W, Joseph-McCarthy D, Wu J, Smith M, Zhang YL, Tam M, Erbe D, Tam S, Saiah E, Lee J, Bioorg Med Chem Lett. 2007 May 15;17(10):2913-20. Epub 2007 Feb 20. PMID:17336064

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