Title of article :
Identification of a monoacid-Based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B
Author/Authors :
Zhili Xin، نويسنده , , Gang Liu، نويسنده , , Cele Abad-Zapatero، نويسنده , , Zhonghua Pei، نويسنده , , Bruce G. Szczepankiewicz، نويسنده , , Xiaofeng Li، نويسنده , , Tianyuan Zhang، نويسنده , , Charles W. Hutchins، نويسنده , , Philip J. Hajduk، نويسنده , , Stephen J. Ballaron، نويسنده , , Michael A. Stashko، نويسنده , , Thomas H. Lubben، نويسنده , , James M. Trevillyan، نويسنده , , Michael R. Jirousek، نويسنده ,
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.
