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微管在细胞的不同进程中起重要的作用,如细胞的新陈代谢、细胞内运输和有丝分裂。以微管为靶点的抗微管药物,是治疗乳腺癌、卵巢癌和肺癌最有效的药物。临床上常用的抗肿瘤药紫杉醇可以促进微管蛋白聚集,抑制肿瘤细胞的快速增殖,但是容易引起多药耐药。新开发的微管稳定剂分为4类:萜类、大环内酯类(如埃坡霉素、伊沙匹隆)、多羟基四烯内酯类和甾类化合物。这些药物与紫杉醇作用机制相似,能对抗由于P糖蛋白外排泵过表达或者微管蛋白突变导致紫杉醇耐药的肿瘤细胞,而且具有良好水溶性。此类药物为治疗癌症提供了新希望。
Microtubules play an important role in different processes of cells, such as cell metabolism, intracellular trafficking and mitosis. Microtubules as a target anti-microtubule drugs, is the treatment of breast cancer, ovarian cancer and lung cancer the most effective drug. Paclitaxel, a commonly used anti-tumor drug in clinic, can promote tubulin aggregation and inhibit the rapid proliferation of tumor cells, but it is easy to cause multi-drug resistance. The newly developed microtubule stabilizers fall into four categories: terpenes, macrolides (such as epothilone, ixabepilone), polyhydroxytetraene lactones and steroids. These drugs, which have a similar mechanism of action to paclitaxel, fight against paclitaxel-resistant tumor cells that are over-expressed by P-glycoprotein efflux pump or tubulin mutation, and have good water solubility. Such drugs offer new hope for the treatment of cancer.