Lee T T, Momparier R L
Med Pediatr Oncol. 1976;2(3):265-70. doi: 10.1002/mpo.2950020307.
5-Azacytidine 5'-triphosphate (5-aza-CTP) inhibited the phosphorylation of uridine, cytidine, and 5-azacytidine (5-aza-C) in a reaction catalyzed by uridine-cytidine kinase. The inhibition appeared to be competitive with respect to the adenosine 5'-triphosphate and noncompetitive with respect to nucleoside substrates. 5-aza-CTP was a potent inhibitor of 5-aza-C phosphorylation but a weak inhibitor of uridine and cytidine phosphorylation. These results suggest that the feedback inhibition of uridine-cytidine kinase by 5-aza-CTP may limit the amount of intracellular nucleotide analog formed in drug-treated cells.
5-氮杂胞苷5'-三磷酸(5-aza-CTP)在尿苷-胞苷激酶催化的反应中抑制尿苷、胞苷和5-氮杂胞苷(5-aza-C)的磷酸化。这种抑制作用对于三磷酸腺苷似乎是竞争性的,而对于核苷底物是非竞争性的。5-aza-CTP是5-aza-C磷酸化的强效抑制剂,但对尿苷和胞苷磷酸化的抑制作用较弱。这些结果表明,5-aza-CTP对尿苷-胞苷激酶的反馈抑制可能会限制药物处理细胞中形成的细胞内核苷酸类似物的量。