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Published on: January 22, 2019
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B
Zhili Xin1, Gang Liu, Cele Abad-Zapatero
1Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6098, USA. zhili.xin@abbott.com
Bioorganic & Medicinal Chemistry Letters
|November 1, 2003
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.

