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A kinetic study of Rhodamine123 pumping by P-glycoprotein

文献类型:期刊论文

作者Wang, Yulin; Hao, DaCheng; Stein, Wilfred D.; Yang, Ling
刊名biochimica et biophysica acta-biomembranes
出版日期2006-10-01
卷号1758期号:10页码:1671-1676
关键词pglycoprotein Rhodamine 123 kinetics resistance fluorescence quenching
产权排序1;1
通讯作者杨凌
英文摘要the mdri p-glycoprotein (p-gp) actively extrudes a wide variety of structurally diverse cytotoxic compounds out of the cell, is widely expressed in the epithelial cells of kidney, liver and intestine, and in the endothelial cells of brain and placenta, and plays an important role in drug resistance. we measured the accumulation of rhodamine 123 (rho 123), a substrate of p-gp, into a drug sensitive and a drug resistant strain of the human leukemia cell line k562, as function of rho123 concentration. with the aid of a mathematical transformation, we used the accumulation of rho123 into the sensitive cells as a surrogate measure for the internal concentration of the probe in the resistant cells, and were thus able to measure the kinetic parameters of drug efflux pumping by p-gp. drug pumping was half-saturated at an external rho123 concentration of 7.2e-06 +/- 1.1e-06 m, and displayed a co-operative behaviour with a hill number of 1.94 +/- 0.32. verapamil could be shown to inhibit rho123 efflux uncompetitively. (c) 2006 elsevier b.v. all rights reserved.
WOS标题词science & technology ; life sciences & biomedicine
类目[WOS]biochemistry & molecular biology ; biophysics
研究领域[WOS]biochemistry & molecular biology ; biophysics
关键词[WOS]nucleotide-binding domains ; drug-binding ; vinblastine ; azidopine ; mechanism ; sites ; cells
收录类别SCI
原文出处true
语种英语
WOS记录号WOS:000241586900012
公开日期2010-11-30
源URL[http://159.226.238.44/handle/321008/97689]  
专题大连化学物理研究所_中国科学院大连化学物理研究所
作者单位1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
2.Hebrew Univ Jerusalem, Inst Life Sci, IL-96263 Jerusalem, Israel
推荐引用方式
GB/T 7714
Wang, Yulin,Hao, DaCheng,Stein, Wilfred D.,et al. A kinetic study of Rhodamine123 pumping by P-glycoprotein[J]. biochimica et biophysica acta-biomembranes,2006,1758(10):1671-1676.
APA Wang, Yulin,Hao, DaCheng,Stein, Wilfred D.,&Yang, Ling.(2006).A kinetic study of Rhodamine123 pumping by P-glycoprotein.biochimica et biophysica acta-biomembranes,1758(10),1671-1676.
MLA Wang, Yulin,et al."A kinetic study of Rhodamine123 pumping by P-glycoprotein".biochimica et biophysica acta-biomembranes 1758.10(2006):1671-1676.

入库方式: OAI收割

来源:大连化学物理研究所

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