脱氧胞苷激酶介导的核苷类似物抗肿瘤药物的现状及前景

Current status and prospects of antitumor nucleoside agents whose activities are mediated by deoxycytidine kinase.

ara- C,CNDAC等核苷类似物药物通过与 DNA链的结合 ,抑制 DNA合成 ,导致细胞死亡 ,从而发挥其抗肿瘤活性 .它们的活化必须借助于脱氧胞苷激酶的磷酸化作用 .本文介绍了此类药物的细胞毒性机制和药物抗性机制的研究进展 。

The nucleoside analogue such as ara\|C and CNDAC exert their antitumor activities through incorporation into DNA strand, inhibiting DNA synthesis and causing the cell kill. In order to be active, they need to be phosphorylated by deoxycytidine kinase. This review discusses the cytotoxic action and resistant mechanism, and introduces some advances in the development of this kind of agents.