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蛋白酪氨酸磷酸酯酶-1B抑制剂的研究进展

Advances in the inhibitors of protein tyrosine phosphatase-1B
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摘要 蛋白酪氨酸磷酸酯酶-1B(PTP-1B)是蛋白酪氨酸磷酸酯酶(PTP)家族中最具代表性的成鼠,因其参与多种生理过程尤其是与机体对胰岛素的敏感性紧密相关,目前已经成为糖尿病和肥胖症治疗的新靶点。现从PTP简介、PTP-1B的结构、生理功能以及6类抑制剂的结构性质等方面进行综述。 As one of the most members in the family of protein tyrosine phosphatases(PTPs),protein tyrosine phosphatase-1B (PTP-1B) plays best-known roles in regulating physiological processes, especially in down regulation of insulin signaling. PTP-1B inhibitors may thus serve as novel medicinal agents for the treatment of type 2 diabetes mellitus and obesity. This article gives an overview of reports that have appeared in the primary scientific literatures on the development of PTP-1B inhibitors,including PTP-1B's structural characteristics and physiological functions as well as the structural properties of six kinds of the PTP inhibitors.
出处 《中国新药杂志》 CAS CSCD 北大核心 2006年第18期1523-1526,共4页 Chinese Journal of New Drugs
基金 国家973计划支持项目(2004CB518902)
关键词 蛋白酪氨酸磷酸酯酶-1B 糖尿病 肥胖症 抑制剂 计算机辅助药物设计 protein tyrosine phosphatase-lB diabetes mellitus obesity inhibitors computer aided drug design
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参考文献22

  • 1陶弢,邹大进.蛋白酪氨酸磷酸酶-1B与肥胖和2型糖尿病[J].国外医学(内分泌学分册),2003,23(5):325-327. 被引量:1
  • 2方红,刘永学.蛋白酪氨酸磷酸酶:治疗前景[J].国外医学(药学分册),2002,29(3):175-177. 被引量:5
  • 3ZHANG ZY.Chemical and mechanistic approaches to the study of protein tyrosine phosphatases[J].Acc Chem Res,2003,36 (6):385-392.
  • 4HOOFT VAN HUIJSDUIJNEN R,SAUER WH,BOMBRUN A,et al.Prospects for inhibitors of protein tyrosine phosphatase 1 B as antidiabetic drugs[J].J Med Chem,2004,47 (17):4142 -4146.
  • 5王淼,邹大进.肥胖与蛋白酪氨酸磷酸酶-1B的研究现状[J].中国临床康复,2004,8(12):2356-2357. 被引量:5
  • 6HUM G,LEE J,TAYLOR SD.Synthesis of difluoro-(3-alkenylphenyl)-methyl]-phosphonic acids on non-crosslinked polystyrene and their evaluation as inhibitors of PTP1B[J].Bioorg Med Chem Lett,2002,12(23):3471-3474.
  • 7LAU CK,BAYLY CI,GAUTHIER JY,et al.Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors[J].Bioorg Med Chem Lett,2004,14 (4):1043-1048.
  • 8LI X,BHANDARI A,HOLMES CP,et al.Alpha,alpha-difluorobeta-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B[J].Bioorg Med Chem Lett,2004,14 (16):4301-4306.
  • 9AHN JH,CHO SY,HA JD,et al.Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents[J].Bioorg Med Chem Lett,2002,12(15):1941 -1946.
  • 10CHEON HG,KIM SM,YANG SD,et al.Discovery of a novel protein tyrosine phosphatase-1B inhibitor,KR61639:potential development as an antihyperglycemic agent[J].Eur J Pharmacol,2004,485 (1/3):333-339.

二级参考文献82

  • 1Forsell P A, Boie Y, Montallhet J, et al. Genomic characterization of the human and mouse protein tyrosine phosphatase-1B genes[J] .Gene,2000,260:145-153.
  • 2Echwald S M, Bach H, Vestergaard H, et 8]. A P387L, variant in protein tyrosine phosphatase-lB(PTP-1B)is associated with type 2 diabetes and impaired serine phosphorylafion of PTP-1B in vitro[J] .Diabetes,2002,51:1-6.
  • 3Mahadev K, Zilberlng A, Zhu L, et al. Insulin-stimulated hydrogen peroxide reversibly inhibits protein-tyrosine phosphatase 1b in vivo and enhances the early insulin action cascede[J] .J Biol Chem,2001,276:21938-21942.
  • 4Tao J,Malbon C C,Wang H Y.Galpha(i2) enhances insulin signaling via suppression of protein- tyrosine phosphatase 1B[J] .J Biol Chem,2001,276:39705-39712.
  • 5Bavichandran L V, Chen H, Li Y, et al. Phosphorylation of PTP 1B at Ser(50) by Akt impairs its ability to dephosphorylate the insulin receptor [ J ]. Mol Endocrinol, 2001,15 :1768-1780.
  • 6Kim J H, Cho H, Ryu S E, et al. Effects of metal ions on the activity of protein tyrosine phosphatase VHR: highly potent and reversible oxidative inactivation by Cu^2+ ion [ J ]. Arch Biochem Biophys,2000,382:72-80.
  • 7Zabolotny J M,Bence-Hanulec K K,et al.PTP-1B regulates leptin signal transduction in vivo[J] . Dev Cell,2002,2:489-495.
  • 8Dadke S, Kusarl A, Kusarl J. Phosphorylation and activation of protein- tyrosine phosphatase(PTP) 1B by insulin receptor[ J]. Mol Cell Biochem,2001,221 : 147-154.
  • 9Wang X Y, Bergdahl K,Heijbel A,et al. Analysis of in vitro interactions of protein- tyrosine phosphatase (PIP) 1B with insulin receptor [ J ]. Mol Cell Endocrinol, 2001,173 : 109-120.
  • 10Venable C L, Frevert E U, Kim Y B, et al. Overexpression of protein- tyrosine phosphatase(PTP) 1B in adipocytes inhibits insulin-stimulated phosphoinositide 3-kinase activity without altering glucose transport or Akffprotein kinase B activation[J] .J Biol Chem, 2000,275 : 18318-18326.

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