1t49

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{{STRUCTURE_1t49| PDB=1t49 | SCENE= }}
{{STRUCTURE_1t49| PDB=1t49 | SCENE= }}
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'''Allosteric Inhibition of Protein Tyrosine Phosphatase 1B'''
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===Allosteric Inhibition of Protein Tyrosine Phosphatase 1B===
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==Overview==
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Obesity and type II diabetes are closely linked metabolic syndromes that afflict &gt;100 million people worldwide. Although protein tyrosine phosphatase 1B (PTP1B) has emerged as a promising target for the treatment of both syndromes, the discovery of pharmaceutically acceptable inhibitors that bind at the active site remains a substantial challenge. Here we describe the discovery of an allosteric site in PTP1B. Crystal structures of PTP1B in complex with allosteric inhibitors reveal a novel site located approximately 20 A from the catalytic site. We show that allosteric inhibitors prevent formation of the active form of the enzyme by blocking mobility of the catalytic loop, thereby exploiting a general mechanism used by tyrosine phosphatases. Notably, these inhibitors exhibit selectivity for PTP1B and enhance insulin signaling in cells. Allosteric inhibition is a promising strategy for targeting PTP1B and constitutes a mechanism that may be applicable to other tyrosine phosphatases.
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{{ABSTRACT_PUBMED_15258570}}
==About this Structure==
==About this Structure==
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[[Category: Allosteric inhibition]]
[[Category: Allosteric inhibition]]
[[Category: Protein tyrosine phosphatase 1b]]
[[Category: Protein tyrosine phosphatase 1b]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:58:48 2008''

Revision as of 03:58, 29 July 2008

Image:1t49.png

Template:STRUCTURE 1t49

Allosteric Inhibition of Protein Tyrosine Phosphatase 1B

Template:ABSTRACT PUBMED 15258570

About this Structure

1T49 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Allosteric inhibition of protein tyrosine phosphatase 1B., Wiesmann C, Barr KJ, Kung J, Zhu J, Erlanson DA, Shen W, Fahr BJ, Zhong M, Taylor L, Randal M, McDowell RS, Hansen SK, Nat Struct Mol Biol. 2004 Aug;11(8):730-7. Epub 2004 Jul 18. PMID:15258570

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