期刊文献+

P-gp及对抗P-gp介导多药耐药的研究现状 被引量:15

Progress in anti-multidrug resistance mediated by p-glycoprotein
下载PDF
导出
摘要 P-糖蛋白在多药耐药中起着重要的作用。本文就P-gp的蛋白结构、作用机制及其与多药耐药的关系以及对抗P-gp介导的MDR的现状做了简要介绍。总之,一方面要继续开发高效的P-gp抑制剂,同时,又要考虑过度抑制P-gp可能会带来不良影响;在抑制P-gp的同时,还要兼顾对其它耐药机制的抑制,只有这样,才能在临床上充分解决多药耐药的问题。 P-glycoprotein (P-gp) plays an important role in multidrug resistance (MDR). This article was focused on the protein structure and the mechanism of P- gp, and especially on the current status in anti-P-gp drug research and discovery. The action of P-gp in MDR was also reviewed. Moreover, the potential adverse reaction of P-gp inhibitors were emphasized since P-gp was involved in the normal function of a lot of organs.
出处 《中国临床药理学与治疗学》 CAS CSCD 2006年第1期14-21,共8页 Chinese Journal of Clinical Pharmacology and Therapeutics
关键词 P-糖蛋白 多药耐药 抑制剂 基因表达 p-glycoprotein multidrug resistance inhibitors gene expression
  • 相关文献

参考文献66

  • 1Murren JR. Modulating multidrug resistance -can we target this therapy[J]? Clin Cancer Res,2002;8:633-5.
  • 2Ambudkar SV, Dey S, Hrycyna CA, Ramachandra M, Pastan I,Gottesman MM. Biochemical, cellular, and pharmacological aspects of the multidrug transporter[J]. Annu Rev Pharmacol Toxicol, 1999;39:361 - 98.
  • 3Zhang JT. The multi-structural feature of the multidrug resistance gene product P-glycoprotein: implications for its mechanism of action (hypothesis) [ J ]. Mol Membr Biol, 2001,18:145 - 52.
  • 4Lin JH, Yamazaki M. Role of P-glycoprotein in pharmacokinetics-clinical implications[J]. Clin Pharmacokinet, 2003;42:59 - 98.
  • 5Loo TW, Bartlett MC, Clarke DM. Substrate-induced conformational changes in the transmembrane segments of human P-glycoprotein. Direct evidence for the substrate-induced fit mechanism for drug binding[ J ]. J Biol Chem, 2003 ;278 : 13603 - 6.
  • 6Loo TW, Clarke DM. Determining the dimensions of the drug-binding domain of human P-glycoprotein using thiol cross-linking compounds as molecular rulers [ J ]. J Biol Chem, 2001 ; 276 :36877 - 80.
  • 7Rosenberg MF, Kamis AB, Callaghan R, Higgins CF, Ford RC.Three-dimensional structures of the mammalian multidrug resistance P-glycoprotein demonstrate major conformational changes in the transmembrane domains upon nucleotide binding [ J]. J Biol Chem, 2003 ; 278 : 8294 - 9.
  • 8Martin C, Berridge G, Higgins CF, Mistry P, Charlton P, Callaghan R. Communication between multiple drug binding sites on P-glycoprotein [ J ]. Mol Phannacol, 2000; 58 : 624 - 32.
  • 9Garrigues A, Loiseau N, Delaforge M, Ferte J, Garrigos M, Andre F, et al. Characterization of two pharmacophores on the multidrug transporter P-glycoprotein [J]. Mol Pharmacol, 2002; 62:1288 - 98.
  • 10Luker GD, Flagg TP, Sha Q, Luker KE, Pica CM, Nichols CG, et al. MDR1 P-glycoprotein reduces influx of substrates without affecting membrane potential[J]. J Biol Chem,2001;276:49053-60.

同被引文献238

引证文献15

二级引证文献50

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部