1pyn
From Proteopedia
(New page: 200px<br /> <applet load="1pyn" size="450" color="white" frame="true" align="right" spinBox="true" caption="1pyn, resolution 2.20Å" /> '''DUAL-SITE POTENT, S...) |
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| - | [[Image:1pyn.gif|left|200px]]<br /> | + | [[Image:1pyn.gif|left|200px]]<br /><applet load="1pyn" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1pyn" size=" | + | |
caption="1pyn, resolution 2.20Å" /> | caption="1pyn, resolution 2.20Å" /> | ||
'''DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE'''<br /> | '''DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A salicylate second site binder was linked to three classes of | + | A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1PYN 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 941 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:// | + | 1PYN 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=941:'>941</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=1PYN OCA]. |
==Reference== | ==Reference== | ||
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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: Liang, H.]] | [[Category: Liang, H.]] | ||
[[Category: Liu, G.]] | [[Category: Liu, G.]] | ||
[[Category: Lubben, T.]] | [[Category: Lubben, T.]] | ||
[[Category: Stashko, M.]] | [[Category: Stashko, M.]] | ||
| - | [[Category: Szczepankiewicz, B | + | [[Category: Szczepankiewicz, B G.]] |
| - | [[Category: Trevillyan, J | + | [[Category: Trevillyan, J M.]] |
[[Category: Zhonghua, P.]] | [[Category: Zhonghua, P.]] | ||
[[Category: 941]] | [[Category: 941]] | ||
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[[Category: protein tyrosine phosphatase inhibited with dual site]] | [[Category: protein tyrosine phosphatase inhibited with dual site]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:33:56 2008'' |
Revision as of 12:34, 21 February 2008
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DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE
Contents |
Overview
A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1PYN 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
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors., Pei Z, Li X, Liu G, Abad-Zapatero C, Lubben T, Zhang T, Ballaron SJ, Hutchins CW, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32. PMID:12951078
Page seeded by OCA on Thu Feb 21 14:33:56 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Abad-Zapatero, C. | Ballaron, S J. | Hajduk, P J. | Liang, H. | Liu, G. | Lubben, T. | Stashko, M. | Szczepankiewicz, B G. | Trevillyan, J M. | Zhonghua, P. | 941 | Malonate-containing inhibitor | Protein tyrosine phosphatase inhibited with dual site
