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1xbo

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Revision as of 21:47, 30 March 2008 by OCA (Talk | contribs)
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Image:1xbo.jpg


PDB ID 1xbo

Drag the structure with the mouse to rotate
, resolution 2.50Å
Ligands:
Gene: PTPN1, PTP1B (Homo sapiens)
Activity: Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Related: 1NL9, 1NNY, 1NO6, 1NZZ, 1ONY, 1ONZ


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



PTP1B complexed with Isoxazole Carboxylic Acid


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.

About this Structure

1XBO is a Single protein structure of sequence from Homo sapiens. 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

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