Your browser doesn't support javascript.
loading
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
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.
Afiliação
  • Xin Z; Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6098, USA. zhili.xin@abbott.com
Bioorg Med Chem Lett ; 13(22): 3947-50, 2003 Nov 17.
Article em En | MEDLINE | ID: mdl-14592481
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.
Assuntos
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas Tirosina Fosfatases / Inibidores Enzimáticos Tipo de estudo: Diagnostic_studies Idioma: En Ano de publicação: 2003 Tipo de documento: Article
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas Tirosina Fosfatases / Inibidores Enzimáticos Tipo de estudo: Diagnostic_studies Idioma: En Ano de publicação: 2003 Tipo de documento: Article