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题名: A kinetic study of Rhodamine123 pumping by P-glycoprotein
作者: Wang, Yulin;  Hao, DaCheng;  Stein, Wilfred D.;  Yang, Ling
通讯作者: 杨凌
关键词: pglycoprotein ;  Rhodamine 123 ;  kinetics ;  resistance ;  fluorescence ;  quenching
刊名: BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
发表日期: 2006-10-01
DOI: 10.1016/j.bbamem.2006.06.004
卷: 1758, 期:10, 页:1671-1676
收录类别: SCI
文章类型: Article
部门归属: 18
项目归属: 1806
产权排名: 1;1
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
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.
关键词[WOS]: NUCLEOTIDE-BINDING DOMAINS ;  DRUG-BINDING ;  VINBLASTINE ;  AZIDOPINE ;  MECHANISM ;  SITES ;  CELLS
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000241586900012
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/97689
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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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

Recommended Citation:
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.
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