作用于微管的抗肿瘤药物研究进展

Progress in Study on the Microtubule-Targeted Anti-Tumor Drugs

微管在有丝分裂及细胞分裂过程中发挥着重要作用,因此许多不同化学结构的抗肿瘤药物都以其为作用靶点。作用于微管的抗肿瘤药物不仅能通过细胞毒作用杀死肿瘤细胞,还可以通过抑制肿瘤血管的功能,使肿瘤细胞无法获得养分死亡而起到抗肿瘤的作用。然而此类药物在临床应用的过程当中也受到了肿瘤细胞产生的耐药性和药物自身毒性的困扰。本文将对作用于微管的抗肿瘤药物的作用机制,耐药性产生的原因以及毒性方面作一综述,以期能够研发出更具针对性、低毒、对耐药机制不敏感的微管抑制剂。

The importance of microtubules in mitosis and cell division makes them a superb target for a group of highly successful, chemically diverse anticancer drugs. Microtubule-targeted anti-tumor drugs not only can induce cell death by cytotoxicity, but also can inhibit the tumor vascular function, then tumor cells generally die without oxygen and nutrients from the blood. In spite of their antitumor activity, innate or acquired drug resistance and toxicity of microtubule-targeted drugs are common, limiting their overall clinical efficacy. We will describe the mechanisms of microtubule-targeted drugs, the reasons for drug resistance and the toxicity of the drugs, hoping microtubule- targeted agents with enhanced tumor specificity, reduced toxicity, and insensitivity to chemo resistance mechanisms will be developed.