Kinetic identification of membrane transporters that assist P-gp mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cells
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word count: 232 (Max limit = 250) Introduction word count: 678 (Max limit = 750) Discussion word count: 1427 (Max limit = 1500) Non-standard Abbreviations: P-gp, the P-glycoprotein product of the hMDR1 gene; A>B (or B>A), transport across the confluent cell monolayer when the donor chamber is apical (or basolateral) and the receiver chamber is basolateral (or apical). This article has not been copyedited and formatted. The final version may differ from this version. DMD Fast Forward. Published on October 29, 2007 as DOI: 10.1124/dmd.107.017301 at A PE T Jornals on Jne 4, 2017 dm d.aspurnals.org D ow nladed from
منابع مشابه
Kinetic identification of membrane transporters that assist P-glycoprotein-mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cells.
A robust screen for compound interaction with P-glycoprotein (P-gp) has some obvious requirements, such as a cell line expressing P-gp and a probe substrate that is transported solely by P-gp and passive permeability. It is actually difficult to prove that a particular probe substrate interacts only with P-gp in the chosen cell line. Using a confluent monolayer of MDCKII-hMDR1 cells, we have de...
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The best parameters for incorporation into mechanistic physiologically based pharmacokinetic models for transporters are system-independent kinetic parameters and active (not total) transporter levels. Previously, we determined the elementary rate constants for P-glycoprotein (P-gp)-mediated transport (on- and off-rate constants from membrane to P-gp binding pocket and efflux rate constant into...
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P-glycoprotein, a human multidrug resistance transporter, has been extensively studied due to its importance to human health and disease. In order to understand transport kinetics via P-gp, confluent cell monolayers overexpressing P-gp are widely used. The purpose of this study is to obtain the mass action elementary rate constants for P-gp's transport and to functionally characterize members o...
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