1qxk

From Proteopedia

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spinqualitylabelsall models PDB ID 1qxk Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image
, resolution 2.30Å
Ligands:
Gene:	PTPN1 OR PTP1B (Homo sapiens)
Activity:	Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Coordinates:	save as pdb, mmCIF, xml

Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

Overview

Monoacid-based PTP1B inhibitors with improved physiochemical properties have been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl mimetic has been linked with an optimized second arylphosphate binding site ligand to produce compound 20 with low micromolar potency against PTP1B, good selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system.

Disease

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

About this Structure

1QXK is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B., Xin Z, Liu G, Abad-Zapatero C, Pei Z, Szczepankiewicz BG, Li X, Zhang T, Hutchins CW, Hajduk PJ, Ballaron SJ, Stashko MA, Lubben TH, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Nov 17;13(22):3947-50. PMID:14592481

Page seeded by OCA on Thu Mar 20 13:44:02 2008