1xbo

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spinqualitylabelsall models 1xbo, resolution 2.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

PTP1B complexed with Isoxazole Carboxylic Acid

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

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 IX1 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

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