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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)
KeywordPglycoprotein Rhodamine 123 Kinetics Resistance Fluorescence Quenching
Source PublicationBIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
2006-10-01
DOI10.1016/j.bbamem.2006.06.004
Volume1758Issue:10Pages:1671-1676
Indexed BySCI
SubtypeArticle
Department18
Funding Project1806
Contribution Rank1;1
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectBiochemistry & Molecular Biology ; Biophysics
WOS Research AreaBiochemistry & Molecular Biology ; Biophysics
WOS KeywordNUCLEOTIDE-BINDING DOMAINS ; DRUG-BINDING ; VINBLASTINE ; AZIDOPINE ; MECHANISM ; SITES ; CELLS
AbstractThe 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.
Language英语
URL查看原文
WOS IDWOS:000241586900012
Citation statistics
Cited Times:25[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/97689
Collection中国科学院大连化学物理研究所
Corresponding AuthorYang L(杨凌)
Affiliation1.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
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,&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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