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1nz7
From Proteopedia
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==Overview== | ==Overview== | ||
| - | We have previously reported a novel series of oxalyl-aryl-amino benzoic | + | 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. |
==Disease== | ==Disease== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Abad-Zapatero, C.]] | [[Category: Abad-Zapatero, C.]] | ||
| - | [[Category: Ballaron, S | + | [[Category: Ballaron, S J.]] |
| - | [[Category: Hajduk, P | + | [[Category: Hajduk, P J.]] |
| - | [[Category: Hutchins, C | + | [[Category: Hutchins, C W.]] |
| - | [[Category: Jirousek, M | + | [[Category: Jirousek, M R.]] |
[[Category: Liu, G.]] | [[Category: Liu, G.]] | ||
[[Category: Lubben, T.]] | [[Category: Lubben, T.]] | ||
| - | [[Category: Oost, T | + | [[Category: Oost, T K.]] |
[[Category: Pei, Z.]] | [[Category: Pei, Z.]] | ||
| - | [[Category: Stashko, M | + | [[Category: Stashko, M A.]] |
| - | [[Category: Szczepankiewicz, B | + | [[Category: Szczepankiewicz, B G.]] |
| - | [[Category: Trevillyan, J | + | [[Category: Trevillyan, J M.]] |
[[Category: Xin, Z.]] | [[Category: Xin, Z.]] | ||
[[Category: 901]] | [[Category: 901]] | ||
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[[Category: protein tyrosine phosphatase fold]] | [[Category: protein tyrosine phosphatase fold]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:11:37 2008'' |
Revision as of 12:11, 21 February 2008
|
POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.
Contents |
Overview
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.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1NZ7 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 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 Thu Feb 21 14:11:37 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Abad-Zapatero, C. | Ballaron, S J. | Hajduk, P J. | Hutchins, C W. | Jirousek, M R. | Liu, G. | Lubben, T. | Oost, T K. | Pei, Z. | Stashko, M A. | Szczepankiewicz, B G. | Trevillyan, J M. | Xin, Z. | 901 | Oxamic acid inhibitor bound to p-loop | Protein tyrosine phosphatase fold
