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1q1m

From Proteopedia

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[[Image:1q1m.jpg|left|200px]]
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{{STRUCTURE_1q1m| PDB=1q1m | SCENE= }}
{{STRUCTURE_1q1m| PDB=1q1m | SCENE= }}
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'''A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors'''
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===A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors===
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==Overview==
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Using an NMR-based fragment screening and X-ray crystal structure-based assembly, starting with millimolar ligands for both the catalytic site and the second phosphotyrosine binding site, we have identified a small-molecule inhibitor of protein tyrosine phosphatase 1B with low micromolar inhibition constant, high selectivity (30-fold) over the highly homologous T-cell protein tyrosine phosphatase, and good cellular activity in COS-7 cells.
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(as it appears on PubMed at http://www.pubmed.gov), where 13678400 is the PubMed ID number.
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{{ABSTRACT_PUBMED_13678400}}
==About this Structure==
==About this Structure==
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[[Category: Protein tyrosine phosphatase 1b]]
[[Category: Protein tyrosine phosphatase 1b]]
[[Category: Ptp1b]]
[[Category: Ptp1b]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:45:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 00:30:14 2008''

Revision as of 21:30, 28 July 2008

Image:1q1m.png

Template:STRUCTURE 1q1m

A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors

Template:ABSTRACT PUBMED 13678400

About this Structure

1Q1M is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor., Liu G, Xin Z, Pei Z, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Zhao H, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR, J Med Chem. 2003 Sep 25;46(20):4232-5. PMID:13678400

Page seeded by OCA on Tue Jul 29 00:30:14 2008

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