Protein tyrosine phosphatase 1B inhibitors for diabetes

被引：574

作者：

Johnson, TO ^{[1
]}

Ermolieff, J ^{[1
]}

Jirousek, MR ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, La Jolla Labs, San Diego, CA 92121 USA

来源：

NATURE REVIEWS DRUG DISCOVERY | 2002年 / 1卷 / 09期

关键词：

D O I：

10.1038/nrd895

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Increased incidence of type 2 diabetes mellitus and obesity has elevated the medical need for new agents to treat these disease states. Resistance to the hormones insulin and leptin are hallmarks of both type 2 diabetes and obesity. Drugs that can ameliorate this resistance should be effective in treating type 2 diabetes and possibly obesity. Protein tyrosine phosphatase 1 B (PTP1B) is thought to function as a negative regulator of insulin and leptin signal transduction. This article reviews PTP1B as a novel target for type 2 diabetes, and looks at the challenges in developing small-molecule inhibitors of this phosphatase.

引用

页码：696 / 709

页数：14

共 93 条

[1] 2-(Oxalylamino)-benzoic acid is a general, competitive inhibitor of protein-tyrosine phosphatases [J].

Andersen, HS ;

Iversen, LF ;

Jeppesen, CB ;

Branner, S ;

Norris, K ;

Rasmussen, HB ;

Moller, KB ;

Moller, NPH .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (10) :7101-7108

[2] Growth models in microporous materials [J].

Anderson, MW ;

Agger, JR ;

Hanif, N ;

Terasaki, O .

MICROPOROUS AND MESOPOROUS MATERIALS, 2001, 48 (1-3) :1-9

[3] The YRD motif is a major determinant of substrate and inhibitor specificity in T-cell protein-tyrosine phosphatase [J].

Asante-Appiah, E ;

Ball, K ;

Bateman, K ;

Skorey, K ;

Friesen, R ;

Desponts, C ;

Payette, P ;

Bayly, C ;

Zamboni, R ;

Scapin, G ;

Ramachandran, C ;

Kennedy, BP .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (28) :26036-26043

[4] CRYSTAL-STRUCTURE OF HUMAN PROTEIN-TYROSINE-PHOSPHATASE 1B [J].

BARFORD, D ;

FLINT, AJ ;

TONKS, NK .

SCIENCE, 1994, 263 (5152) :1397-1404

[5] The mechanism of protein kinase regulation by protein phosphatases [J].

Barford, D .

BIOCHEMICAL SOCIETY TRANSACTIONS, 2001, 29 :385-391

[6]

BAYTY C, 2001, Patent No. [00170754, 0170754]

[7]

BIETH JG, 1995, METHOD ENZYMOL, V248, P59

[8]

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

[9] 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

[10] Regulated transport of the glucose transporter glut4 [J].

Bryant, NJ ;

Govers, R ;

James, DE .

NATURE REVIEWS MOLECULAR CELL BIOLOGY, 2002, 3 (04) :267-277

← 1 2 3 4 5 6 7 8 9 10 →