1nz7

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[[Image:1nz7.jpg|left|200px]]
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{{STRUCTURE_1nz7| PDB=1nz7 | SCENE= }}
{{STRUCTURE_1nz7| PDB=1nz7 | SCENE= }}
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'''POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.'''
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===POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.===
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==Overview==
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We have previously reported a novel series of oxalyl-aryl-amino benzoic acid-based, catalytic site-directed, competitive, reversible protein tyrosine phosphatase 1B (PTP1B) inhibitors. With readily access to key intermediates, we utilized a solution phase parallel synthesis approach and rapidly identified a highly potent PTP1B inhibitor (19, K(i)=76 nM) with moderate selectivity (5-fold) over T-cell PTPase (TCPTP) through interacting with a second phosphotyrosine binding site (site 2) in the close proximity to the catalytic site.
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(as it appears on PubMed at http://www.pubmed.gov), where 12749891 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12749891}}
==About this Structure==
==About this Structure==
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[[Category: Oxamic acid inhibitor bound to p-loop]]
[[Category: Oxamic acid inhibitor bound to p-loop]]
[[Category: Protein tyrosine phosphatase fold]]
[[Category: Protein tyrosine phosphatase fold]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 03:09:55 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:51:19 2008''

Revision as of 06:51, 29 July 2008

Image:1nz7.png

Template:STRUCTURE 1nz7

POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.

Template:ABSTRACT PUBMED 12749891

About this Structure

1NZ7 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Potent, selective inhibitors of protein tyrosine phosphatase 1B., Xin Z, Oost TK, Abad-Zapatero C, Hajduk PJ, Pei Z, Szczepankiewicz BG, Hutchins CW, Ballaron SJ, Stashko MA, Lubben T, Trevillyan JM, Jirousek MR, Liu G, Bioorg Med Chem Lett. 2003 Jun 2;13(11):1887-90. PMID:12749891

Page seeded by OCA on Tue Jul 29 09:51:19 2008

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