ALKYLATING AND PLATINUM-BASED AGENTS
ALKYLATING AND PLATINUM-BASED AGENTS
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DOI：
10.1097/00001622-199012000-00014
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发表时间：
1990-01-01
影响因子：
3.4
通讯作者：
EASTMAN A
中科院分区：
文献类型：
--
作者：
EASTMAN A
烷化剂和铂配位络合物代表了用于几乎所有肿瘤的治疗药物的主要部分。烷化剂在肿瘤化疗的发展中起着重要的作用。氮芥氮芥是从第一次世界大战中使用的硫芥子气演变而来的，是第一个在人类中显示出显着抗肿瘤活性的非激素药物。烷化剂通过烷基与细胞大分子的共价结合而起作用。DNA被认为是关键靶点;也许最好的证据是DNA修复缺陷细胞突变体对这类药物的敏感性增强。顺铂不被定义为烷基化剂，因为它缺乏烷基。然而，它与DNA的反应方式类似于烷化剂，在所有其他方面，其作用机制是相同的。
Alkylating agents and platinum coordination complexes represent a major part of the therapeutic armamentarium used against almost all tumors. The alkylating agents played an important role in the development of cancer chemotherapy. The nitrogen mustard mechlorethamine evolved from sulfur mustard gas used in World War 1, and was the first nonhormonal agent to show significant antitumor activity in humans. The alkylating agents act through the covalent binding of alkyl groups to cellular macromolecules. DNA is considered the critical target; perhaps the best evidence for this is the enhanced sensitivity of DNA-repair-defkient cell mutants to this class of agents. Cis-platin is not defined as an alkylating agent because it lacks the alkyl group. However, it reacts with DNA in a manner analogous to alkylating agents, and in all other respects its mechanism of action is the same.