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Aliphatic Chain Length Specificity of the Polyamine Transport System in Ascites L1210 Leukemia Cells¹

Grace Cancer Drug Center, Roswell Park Memorial Institute, Buffalo, New York 14263 [C. W. P., J. M.], and Department of Medicinal Chemistry, J. Hillis Miller Health Center, University of Florida, Gainesville, Florida 32610 [R. J. B.]

A series of diamine homologues of putrescine and triamine homologues of spermidine was used to determine the structural specificity of the polyamine transport system in ascites L1210 leukemia cells by measuring their ability to compete with [³H]-putrescine, [³H]spermidine, or [³H]spermine for uptake. Transport specificity among the diamines (as indicated by K_i constants) was greatest for those having chain lengths similar to that of spermidine and least for those similar to putrescine. Among the triamines, transport specificity was greatest for those having an overall chain length similar to those of spermidine and spermine. The homologue competition profiles were relatively the same for [³H]putrescine, [³H]spermidine, or [³H]spermine, suggesting that all three polyamines utilize the same transport system. This was further substantiated by uptake kinetic plots which showed that the three polyamines were competitive inhibitors of one another. In terms of receptor specificity, the ranking order among the polyamines was as follows: spermine (apparent K_m, 1.6 µM) > spermidine (apparent K_m, 2.2 µM) > putrescine (apparent K_m, 8.5 µM). This information should prove useful in designing anticancer agents which are intended to utilize this transport system.

¹ This investigation was supported by Grants CA-22153, CA-33321, CA-24538, and CA-13038 from the National Cancer Institute, Department of Health, Education, and Welfare.

² To whom requests for reprints should be addressed.

Received 6/20/83. Accepted 9/28/83.

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