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通过分子和生化药理学研究已鉴别出许多抗癌药物的新分子靶 ,微管被认为是癌症化疗的重要的分子靶之一。作用于微管的药物可分为两类 :紫杉烷类 (紫杉醇、docetax el)及长春花生物碱类 ,前者促进微管的聚合并提高其稳定性 ,后者及rhizoxin则抑制微管的聚合 ,两类生物碱均干扰微管的功能 (细胞能动性、细胞内转运以及有丝分裂等 )。影响这两类生物碱药效的因素有 :药物的细胞内蓄积、微管蛋白的遗传学改变、微管蛋白的合成、微管蛋白的药物结合能力、药物的代谢灭活以及微管相关蛋白的改变等
A new molecular target of many anticancer drugs has been identified through molecular and biochemical pharmacological studies. Microtubules are considered as one of the important molecular targets for cancer chemotherapy. Drugs that act on microtubules can be divided into two categories: taxanes (docetaxel) and vinca alkaloids, the former to promote the polymerization of microtubules and increase their stability, the latter and rhizoxin inhibit microtubule Polymerization, both alkaloids interfere with microtubule functions (cell motility, intracellular transport and mitosis, etc.). Factors that affect the efficacy of these two alkaloids are: intracellular accumulation of drugs, genetic changes in tubulin, tubulin synthesis, tubulin drug binding capacity, drug metabolism inactivation, and microtubule-associated proteins Change and so on