Enhancement of Antitumor Activity of Glutamine Antagonists 6-Diazo-5-oxo-l-norleucine and Acivicin in Cell Culture by Glutaminase-Asparaginase
作者： Joseph Roberts , Henry Rosenfeld
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摘要: Abstract Mouse P388 and L1210 leukemia cells grown in vitro were found to be 4 10 times more sensitive 6-diazo-5-oxo-l-norleucine 3 5 Acivicin than 3T3 C57BL × DBA/2 F 1 embryonic fibroblasts. The combined actions of succinylated Acinetobacter glutaminase-asparaginase or produced synergistic inhibition nucleic acid synthesis tumor cells. An uptake system for is described. Its properties are similar their strong temperature dependence, utilization the “L” transport system, presumably competitive by glutamine, K m 9s (about 200 µm), potent p-chloromercuribenzene sulfonate, Na + . However, was inhibited (but not P388) KCN 2,4-dinitrophenol. At equilibrium cells, intracellular level approximately 57-fold greater extracellular concentration. accumulated metabolized nor does exchange H label into water occur. Rapid efflux occurred with both cell lines at 37°, but from greatly diminished 0°. rate accelerated including glutamine unlabeled medium.
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