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DNA结合的抗肿瘤药物是一类重要的肿瘤化疗剂。他们的共同特征是与肿瘤细胞的DNA结合,从而干扰DNA的复制和RNA的合成,使肿瘤细胞遭受致死性损伤。按其与DNA的结合方式,可将这类药物再分成嵌入和非嵌入两种类型。非嵌入型的DNA-结合药物先结合于DNA小沟(Minor groove),然后与DNA分子共价结合,导致染色体破裂而干扰肿瘤细胞DNA的复制。属于这类药物的博莱霉素(Bleomycin)、链黑霉素(Streptonigrin)安拉霉素(Anthramycin)等抗肿瘤抗生素具有良好的抗肿瘤活性,产生的细胞毒效果可与烷化剂匹配。嵌入型的DNA-结合药物嵌入DNA的碱基对,阻断依赖DNA的RNA
DNA-bound antitumor drugs are a class of important oncology chemotherapeutic agents. Their common feature is the DNA binding of tumor cells, thus interfering with DNA replication and RNA synthesis, causing tumor cells to suffer lethal damage. According to its combination with the DNA, these drugs can be subdivided into two types of embedded and non-embedded. Non-embedded DNA-binding drugs first bind to the minor groove and then covalently bind to the DNA molecule, causing the chromosome to rupture and interfering with DNA replication in the tumor cells. The antitumor antibiotics such as Bleomycin, Streptonigrin and Anthramycin which belong to these drugs have good anti-tumor activity and the cytotoxic effect produced can be matched with the alkylating agent. Embedded DNA-binding drugs insert DNA base pairs that block DNA-dependent RNA