Kinetic analysis of active efflux of vincristine from multidrug-resistant P388 leukemia cells.

Kinetic analysis of active efflux of vincristine from multidrug-resistant P388 leukemia cells.
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多重耐药 P388 白血病细胞长春新碱主动流出的动力学分析。

DOI:
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发表时间:
1987
期刊:
Japanese journal of cancer research : Gann
影响因子:
--
通讯作者:
Yuichi Sugiyama
Yuichi Sugiyama
中科院分区:
--
文献类型:
--
作者:
Makoto Inaba;Tohru Watanabe;Yuichi Sugiyama

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Kinetic analysis of vincristine transport in parental and multidrug-resistant P388 leukemia cells was attempted by indirect assessment of its efflux. Practically, the initial velocity and steady-state level of vincristine uptake by ATP-depleted cells, and its steady-state level in untreated cells, were measured. As a result, a saturable process of not only influx but also efflux of vincristine was observed for the first time with both cell lines, suggesting the existence of a carrier-mediated system for influx and efflux. With increasing extracellular drug concentrations, the contribution of the mediated transport to the total flux was decreased and that of the unsaturable process, that is, simple diffusion, was increased. It should be particularly noted that the Km and Vmax values of efflux in the resistant cells were significantly less and greater, respectively, than those of the sensitive cells, providing a biochemical basis for enhanced efflux as a mechanism of multidrug-resistance. No significant difference in kinetic parameters of vincristine influx and intracellular binding contributing to resistance was found between the two cell lines.
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DOI: 10.1159/000137945
发表时间: 1984
期刊: Pharmacology
影响因子: 3.1
作者:
Sugiyama,Y;Kaplowitz,N
通讯作者: Kaplowitz,N
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发表时间: 1995
期刊: The Journal of biological chemistry
影响因子: --
作者:
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DOI: --
发表时间: 1983
影响因子: 3.6
作者:
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