Inhibition of DNA-dependent DNA polymerase α by arabinosyl-5-azacytosine and its metabolic transformation in L1210 mouse leukemic cells
1986 ◽
Vol 51
(10)
◽
pp. 2285-2290
Keyword(s):
Arabinosyl-5-azacytosine is phosphorylated by the L1210 mouse leukemic cells in vivo as well as by the cell-free extract in the presence of ATP. The drug inhibits in vitro the activity of DNA-dependent DNA polymerase α from L1210 cells in a dose-dependent manner but to a lesser degree than arabinosylcytosine. When administered in vivo, it depresses the activity of DNA polymerase to about the same extent as arabinosylcytosine. The Km constant for the phosphorylation of arabinosyl-5-azacytosine is 46% higher than the corresponding value for arabinosylcytosine.