Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates

被引：35

作者：

Zloh, M

Kaatz, GW

Gibbons, S

机构：

[1] Univ London, Sch Pharm, Dept Pharmaceut & Biol Chem, London WC1N 1AX, England

[2] Univ London, Sch Pharm, Ctr Pharmacognosy & Phytotherapy, London WC1N 1AX, England

[3] Wayne State Univ, Sch Med, Dept Internal Med, Div Infect Dis, Detroit, MI 48201 USA

[4] John D Dingell Dept Vet Affairs Med Ctr, Detroit, MI 48201 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 04期

关键词：

MDR; multidrug-resistance; molecular modelling; mechanism; bacteria; tumour;

D O I：

10.1016/j.bmcl.2003.12.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Multidrug-resistance (MDR) occurs in many bacterial species and tumour cells. MDR functions by membrane proteins which export drugs from cells, resulting in a low ineffective concentration of the drug. We have shown by molecular modelling that inhibitors of MDR have affinity for substrates of MDR transporters. This affinity may facilitate drug entry into cells and a large inhibitor-drug complex may be a poorer substrate for the MDR mechanism. This complex would effectively 'cloak' the drug rendering it unavailable for efflux. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：881 / 885

页数：5

共 26 条

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