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

[11] Steric hindrance as a basis for structure-based design of selective inhibitors of protein-tyrosine phosphatases [J].

Iversen, LF ;

Andersen, HS ;

Moller, KB ;

Olsen, OH ;

Peters, GH ;

Branner, S ;

Mortensen, SB ;

Hansen, TK ;

Lau, J ;

Ge, Y ;

Holsworth, DD ;

Newman, NJ ;

Moller, NPH .

BIOCHEMISTRY, 2001, 40 (49) :14812-14820

[12] Protein tyrosine phosphatase 1B inhibitors for diabetes [J].

Johnson, TO ;

Ermolieff, J ;

Jirousek, MR .

NATURE REVIEWS DRUG DISCOVERY, 2002, 1 (09) :696-709

[13] Increased energy expenditure, decreased adiposity, and tissue-specific insulin sensitivity in protein-tyrosine phosphatase 1B-deficient mice [J].

Klaman, LD ;

Boss, O ;

Peroni, OD ;

Kim, JK ;

Martino, JL ;

Zabolotny, JM ;

Moghal, N ;

Lubkin, M ;

Kim, YB ;

Sharpe, AH ;

Stricker-Krongrad, A ;

Shulman, GI ;

Neel, BG ;

Kahn, BB .

MOLECULAR AND CELLULAR BIOLOGY, 2000, 20 (15) :5479-5489

[14] PROTEIN-TYROSINE-PHOSPHATASE INHIBITION BY A PEPTIDE-CONTAINING THE PHOSPHOTYROSYL MIMETIC, L-O-MALONYLTYROSINE [J].

KOLE, HK ;

AKAMATSU, M ;

YE, B ;

YAN, XJ ;

BARFORD, D ;

ROLLER, PP ;

BURKE, TR .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1995, 209 (03) :817-822

[15] Synthesis and biological activity of a novel class of small molecular weight peptidomimetic competitive inhibitors of protein tyrosine phosphatase 1B [J].

Larsen, SD ;

Barf, T ;

Liljebris, C ;

May, PD ;

Ogg, D ;

O'Sullivan, TJ ;

Palazuk, BJ ;

Schostarez, HJ ;

Stevens, FC ;

Bleasdale, JE .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (03) :598-622

[16]

LIU G, 2003, J MED CHEM 0625

[17]

Liu Gang, 2002, Curr Opin Investig Drugs, V3, P1608

[18] Protein tyrosine phosphatases in signal transduction [J].

Neel, BG ;

Tonks, NK .

CURRENT OPINION IN CELL BIOLOGY, 1997, 9 (02) :193-204

[19]

Nilsson I, 2000, Prog Cell Cycle Res, V4, P107

[20] CD45: new jobs for an old acquaintance [J].

Penninger, JM ;

Irie-Sasaki, J ;

Sasaki, T ;

Oliveira-dos-Santos, AJ .

NATURE IMMUNOLOGY, 2001, 2 (05) :389-396

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