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- W1569512397 abstract "Comparison was made of the uptake in L1210 leukemia cells of the agents aminopterin, methotrexate, and the quinazoline antifolate methasquin. Intracellular drug content was measured by titration with a bacterial dihydrofolate reductase. All three agents gain entry into the cell by carrier-mediated transport, since uptake is temperature dependent, saturable, and concentrative. Of the three drugs, aminopterin is transported most efficiently. At the same rate-limiting external concentration, the transport of methotrexate is one-fourth as efficient as that of aminopterin and the transport of methasquin is one-twentieth as efficient. Differences in the ability of the three drugs to be transported, as indicated by the respective Michaelis constants for initial uptake velocity, seem related to a difference in the affinity of a carrier component for each drug. All three drugs appear to be transported by the same mechanism, since competition for the same carrier component among the three drugs, as well as between them and the normal analogs, folate and folinate, was demonstrated with the expected quantitative relationships. The rate of efflux of aminopterin and methotrexate from the L1210 cell is far greater than the rate for methasquin. The extent of concentrative uptake during influx (uptake) of aminopterin is somewhat higher than that for methotrexate or methasquin at a rate-limiting concentration for influx." @default.
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- W1569512397 date "1972-10-01" @default.
- W1569512397 modified "2023-09-23" @default.
- W1569512397 title "Comparative studies on the transport of aminopterin, methotrexate, and methasquin by the L1210 leukemia cell." @default.
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