2b07

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Image:2b07.gif


PDB ID 2b07

Drag the structure with the mouse to rotate
, resolution 2.1Å
Ligands:
Gene: PTPN1, PTP1B (Homo sapiens)
Activity: Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Coordinates: save as pdb, mmCIF, xml



Crystal structure of PTP1B with Tricyclic Thiophene inhibitor.


Contents

Overview

A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening of phosphotyrosine mimics at high micromolar concentrations. The potency of this lead compound has been improved significantly by medicinal chemistry guided by X-ray crystallography and molecular modeling. Excellent consistency has been observed between structure-activity relationships and structural information from PTP1B-inhibitor complexes.

Disease

Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]

About this Structure

2B07 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors., Moretto AF, Kirincich SJ, Xu WX, Smith MJ, Wan ZK, Wilson DP, Follows BC, Binnun E, Joseph-McCarthy D, Foreman K, Erbe DV, Zhang YL, Tam SK, Tam SY, Lee J, Bioorg Med Chem. 2006 Apr 1;14(7):2162-77. Epub 2005 Nov 21. PMID:16303309

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