Title of article
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors
Author/Authors
Baolin Wu&Hongyu Zhao، نويسنده , , Gang Liu، نويسنده , , Zhili Xin، نويسنده , , Michael D. Serby، نويسنده , , Zhonghua Pei، نويسنده , , Bruce G. Szczepankiewicz، نويسنده , , Philip J. Hajduk، نويسنده , , Cele Abad-Zapatero، نويسنده , , Charles W. Hutchins، نويسنده , , Thomas H. Lubben، نويسنده , , Stephen J. Ballaron، نويسنده , , Deanna L. Haasch، نويسنده , , Wiweka Kaszubska، نويسنده , , Cristina M. Rondinone، نويسنده , , James M. Trevillyan، نويسنده , , Michael R. Jirousek، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
5543
To page
5546
Abstract
Guided by X-ray crystallography, we have extended the structure–activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.
Keywords
e-mail: hongyu.zhao@abbott.com , PTP1B , Cell permeable.* Corresponding author. Tel.: +1 847 935 4566 , Selective , fax: +1 847 9381674
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795020
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