Recent advances in protein tyrosine phosphatase 1B inhibitors

被引:75
作者
Taylor, SD [1 ]
Hill, B [1 ]
机构
[1] Univ Waterloo, Dept Chem, Waterloo, ON N2L 3G1, Canada
关键词
inhibitors; obesity; protein tyrosine phosphatases; PTP1B; Type; 2; diabetes;
D O I
10.1517/eoid.13.3.199.27347
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Type 2 diabetes and obesity are characterised by insulin and leptin resistance. Studies suggest that these may be due to defects in the insulin and, leptin signalling pathways. Over the last decade, a considerable body of evidence has been amassed indicating that protein tyrosine phosphatase 1B (PTP1B) is involved in the downregulation of insulin and leptin signalling. Consequently, compounds that inhibit PrP1B have potential as therapeutics for treating Type 2 diabetes and obesity. This review covers recent advances in PTP1B inhibitors with an emphasis on recent attempts to create potent, selective and cell-permeable small-molecule inhibitors.
引用
收藏
页码:199 / 214
页数:16
相关论文
共 90 条
[1]   INCREASED ABUNDANCE OF SPECIFIC SKELETAL-MUSCLE PROTEIN-TYROSINE PHOSPHATASES IN A GENETIC MODEL OF INSULIN-RESISTANT OBESITY AND DIABETES-MELLITUS [J].
AHMAD, F ;
GOLDSTEIN, BJ .
METABOLISM-CLINICAL AND EXPERIMENTAL, 1995, 44 (09) :1175-1184
[2]   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
[3]   Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B [J].
Andersen, HS ;
Olsen, OH ;
Iversen, LF ;
Sorensen, ALP ;
Mortensen, SB ;
Christensen, MS ;
Branner, S ;
Hansen, TK ;
Lau, JF ;
Jeppesen, L ;
Moran, EJ ;
Su, J ;
Bakir, F ;
Judge, L ;
Shahbaz, M ;
Collins, T ;
Vo, T ;
Newman, MJ ;
Ripka, WC ;
Moller, NPH .
JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (20) :4443-4459
[4]   The structure of PTP-1B in complex with a peptide inhibitor reveals an alternative binding mode for bisphosphonates [J].
Asante-Appiah, E ;
Patel, S ;
Dufresne, C ;
Roy, P ;
Wang, QP ;
Patel, V ;
Friesen, RW ;
Ramachandran, C ;
Becker, JW ;
Leblanc, Y ;
Kennedy, BP ;
Scapin, G .
BIOCHEMISTRY, 2002, 41 (29) :9043-9051
[5]   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
[6]   Protein-tyrosine phosphatase 1B complexes with the insulin receptor in vivo and is tyrosine-phosphorylated in the presence of insulin [J].
Bandyopadhyay, D ;
Kusari, A ;
Kenner, KA ;
Liu, F ;
Chernoff, J ;
Gustafson, TA ;
Kusari, J .
JOURNAL OF BIOLOGICAL CHEMISTRY, 1997, 272 (03) :1639-1645
[7]   CRYSTAL-STRUCTURE OF HUMAN PROTEIN-TYROSINE-PHOSPHATASE 1B [J].
BARFORD, D ;
FLINT, AJ ;
TONKS, NK .
SCIENCE, 1994, 263 (5152) :1397-1404
[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]   Dynamics of the interaction between the insulin receptor and protein tyrosine-phosphatase 1B in living cells [J].
Boute, N ;
Boubekeur, S ;
Lacasa, D ;
Issad, T .
EMBO REPORTS, 2003, 4 (03) :313-319