DICP OpenIR
学科主题物理化学
A Kinetic Study of Rhodamine 123 Pumping by P-glycoprotein
Yang L(杨凌); Wang YL(王玉林); WilfredD.Stein
会议名称The 1st asia Pacific ISSX Meeting
会议日期2006-5-24
2006-05-24
会议地点韩国
页码271/1
部门归属十八室
英文摘要Objective: To understand the transport kinetics of P-glycoprotein with detail. Methods: We have developed a kinetic approach to study P-gp transport, based on the influx of Rhodamine 123 (Rho123), a much-used probe for P-gp. In order to avoid the complications in data analysis that can arise due to the self-quenching of Rho123 within the loaded cells, we introduce a method in which the drug sensitive cells are used to provide a calibration curve for the amount of Rho123 accumulated within the cells at any level of external probe (upper curve, figure A, below). This enables us to calculate, for the resistant cells (lower curve, in A), the relative amount of probe that has been pumped out of the cells. Results and conclusion: We use this to obtain a measure of the fraction of the probe that is pumped out of the cell, at any level of external Rho123 (Curve B in figure). It is from this fraction and its dependence on the level of external probe that we derive the kinetic data for Rho123 pumping. We confirm that P-gp is an effective efflux transporter of Rho123 and that there is co-operative interaction between Rho123 molecules (probably in pairs, the Hill number being 1.94+/- 0.32) as they bind to P-gp during efflux pumping. We estimate the apparent affinity of Rho123 for the pump’s binding sites as Km = 7.2 +/- 1.1 uM. Verapamil addition diminishes the rate of efflux pumping, with Ki = 1.1 uM, and does so in an un-competitive fashion. (Supported by the DUT-DICP scientific cooperation fund)
语种中文
WOS记录号WOS:000242406900252
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被引频次:3[WOS]   [WOS记录]     [WOS相关记录]
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/112190
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Yang L,Wang YL,WilfredD.Stein. A Kinetic Study of Rhodamine 123 Pumping by P-glycoprotein[C],2006:271/1.
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