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Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.

Authors
  • Xin, Zhili
  • Liu, Gang
  • Abad-Zapatero, Cele
  • Pei, Zhonghua
  • Szczepankiewicz, Bruce G
  • Li, Xiaofeng
  • Zhang, Tianyuan
  • Hutchins, Charles W
  • Hajduk, Philip J
  • Ballaron, Stephen J
  • Stashko, Michael A
  • Lubben, Thomas H
  • Trevillyan, James M
  • Jirousek, Michael R
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Nov 17, 2003
Volume
13
Issue
22
Pages
3947–3950
Identifiers
PMID: 14592481
Source
Medline
License
Unknown

Abstract

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.

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