1xbo
From Proteopedia
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==Overview== | ==Overview== | ||
| - | Guided by X-ray crystallography, we have extended the structure-activity | + | Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells. |
==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: Hassach, D | + | [[Category: Hassach, D L.]] |
| - | [[Category: Hutchins, C | + | [[Category: Hutchins, C W.]] |
| - | [[Category: Jirousek, M | + | [[Category: Jirousek, M R.]] |
[[Category: Kaszubska, W.]] | [[Category: Kaszubska, W.]] | ||
[[Category: Liu, G.]] | [[Category: Liu, G.]] | ||
| - | [[Category: Lubben, T | + | [[Category: Lubben, T H.]] |
[[Category: Pei, Z.]] | [[Category: Pei, Z.]] | ||
| - | [[Category: Rondinone, C | + | [[Category: Rondinone, C M.]] |
[[Category: Serby, M.]] | [[Category: Serby, M.]] | ||
| - | [[Category: Szczepankiewicz, B | + | [[Category: Szczepankiewicz, B G.]] |
| - | [[Category: Trevillyan, J | + | [[Category: Trevillyan, J M.]] |
[[Category: Xin, Z.]] | [[Category: Xin, Z.]] | ||
[[Category: Zhao, H.]] | [[Category: Zhao, H.]] | ||
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[[Category: ptp1b]] | [[Category: ptp1b]] | ||
| - | ''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 15:53:02 2008'' |
Revision as of 13:53, 21 February 2008
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PTP1B complexed with Isoxazole Carboxylic Acid
Contents |
Overview
Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1XBO 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
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors., Zhao H, Liu G, Xin Z, Serby MD, Pei Z, Szczepankiewicz BG, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2004 Nov 15;14(22):5543-6. PMID:15482920
Page seeded by OCA on Thu Feb 21 15:53:02 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Abad-Zapatero, C. | Ballaron, S J. | Hajduk, P J. | Hassach, D L. | Hutchins, C W. | Jirousek, M R. | Kaszubska, W. | Liu, G. | Lubben, T H. | Pei, Z. | Rondinone, C M. | Serby, M. | Szczepankiewicz, B G. | Trevillyan, J M. | Xin, Z. | Zhao, H. | IX1 | Isoxazole carboxylic acid | Protein tyrosine phosphatase 1b | Ptp1b
