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A kinetic study of Rhodamine123 pumping by P-glycoprotein
Wang, Yulin; Hao, DaCheng; Stein, Wilfred D.; Yang, Ling; Yang L(杨凌)
关键词Pglycoprotein Rhodamine 123 Kinetics Resistance Fluorescence Quenching
刊名BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
2006-10-01
DOI10.1016/j.bbamem.2006.06.004
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
关键词[WOS]NUCLEOTIDE-BINDING DOMAINS ; DRUG-BINDING ; VINBLASTINE ; AZIDOPINE ; MECHANISM ; SITES ; CELLS
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.
语种英语
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WOS记录号WOS:000241586900012
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被引频次:23[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/97689
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
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
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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,&杨凌.(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.
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