Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors

被引：27

作者：

Pei, ZH

Li, XF

Liu, G

Abad-Zapatero, C

Lubben, T

Zhang, TY

Ballaron, SJ

Hutchins, CW

Trevillyan, JM

Jirouseka, MR

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Metab Dis Res, Abbott Pk, IL 60064 USA

[2] Abbott Labs, Global Pharmaceut Res & Dev, Adv Technol, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(03)00725-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3129 / 3132

页数：4

共 28 条

[1] The structure and mechanism of protein phosphatases: Insights into catalysis and regulation [J].

Barford, D ;

Das, AK ;

Egloff, MP .

ANNUAL REVIEW OF BIOPHYSICS AND BIOMOLECULAR STRUCTURE, 1998, 27 :133-164

[2] PURIFICATION AND CRYSTALLIZATION OF THE CATALYTIC DOMAIN OF HUMAN PROTEIN-TYROSINE-PHOSPHATASE 1B EXPRESSED IN ESCHERICHIA-COLI [J].

BARFORD, D ;

KELLER, JC ;

FLINT, AJ ;

TONKS, NK .

JOURNAL OF MOLECULAR BIOLOGY, 1994, 239 (05) :726-730

[3]

Blaskovich MA, 2002, EXPERT OPIN THER PAT, V12, P871

[4] Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin actions [J].

Bleasdale, JE ;

Ogg, D ;

Palazuk, BJ ;

Jacob, CS ;

Swanson, ML ;

Wang, XY ;

Thompson, DP ;

Conradi, RA ;

Mathews, WR ;

Laborde, AL ;

Stuchly, CW ;

Heijbel, A ;

Bergdahl, K ;

Bannow, CA ;

Smith, CW ;

Svensson, C ;

Liljebris, C ;

Schostarez, HJ ;

May, PD ;

Stevens, FC ;

Larsen, SD .

BIOCHEMISTRY, 2001, 40 (19) :5642-5654

[5]

Burke TR, 1998, BIOPOLYMERS, V47, P225, DOI 10.1002/(SICI)1097-0282(1998)47:3<225::AID-BIP3>3.0.CO

[6]

2-O

[7] Coordinated action of protein tyrosine phosphatases in insulin signal transduction [J].

Cheng, A ;

Dubé, N ;

Gu, F ;

Tremblay, ML .

EUROPEAN JOURNAL OF BIOCHEMISTRY, 2002, 269 (04) :1050-1059

[8]

ECHEBLY M, 1999, SCIENCE, V283, P1544

[9] Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains [J].

Gao, Y ;

Wu, L ;

Luo, JH ;

Guo, R ;

Yang, D ;

Zhang, ZY ;

Burke, TR .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (09) :923-927

[10] Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif [J].

Gao, Y ;

Voigt, J ;

Zhao, H ;

Pais, GCG ;

Zhang, XC ;

Wu, L ;

Zhang, ZY ;

Burke, TR .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (18) :2869-2878

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