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
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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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