1nz7
From Proteopedia
(New page: 200px<br /> <applet load="1nz7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1nz7, resolution 2.40Å" /> '''POTENT, SELECTIVE I...) |
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caption="1nz7, resolution 2.40Å" /> | caption="1nz7, resolution 2.40Å" /> | ||
'''POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.'''<br /> | '''POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1NZ7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 901 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http:// | + | 1NZ7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=901:'>901</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NZ7 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: protein tyrosine phosphatase fold]] | [[Category: protein tyrosine phosphatase fold]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:31:29 2008'' |
Revision as of 14:31, 15 February 2008
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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 Fri Feb 15 16:31:29 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
