Niitani H, Hisakatsu S
Forth Dept. of Internal Medicine, Nippon Medical School.
Gan To Kagaku Ryoho. 1993 Jan;20(1):34-41.
Microtubules are among the most strategic subcellular targets of anticancer agents. Recently, new antimicrotubule agents have been introduced to clinical cancer chemotherapy. Navelbine is a new derivative of vinca alkaloids, which especially has an activity against NSCLC. Unlike classical anti-microtubules agents like colchitine and vinca alkaloids, which induce depolymerization of microtubules, taxol has an unique mechanism of action which induces tubulin polymerization. Taxotere, an analogue of taxol is slightly more active as a promoter of tubulin polymerization than Taxol. E7010 is a novel sulfonamide that inhibits tubulin polymerization. Results of preclinical and clinical studies of these agents are reviewed.
微管是抗癌药物最具针对性的亚细胞靶点之一。近来,新型抗微管药物已应用于临床癌症化疗。诺维本是长春花生物碱的一种新衍生物,尤其对非小细胞肺癌有活性。与秋水仙碱和长春花生物碱等经典抗微管药物诱导微管解聚不同,紫杉醇有独特的作用机制,可诱导微管蛋白聚合。泰索帝是紫杉醇的类似物,作为微管蛋白聚合促进剂,其活性略高于紫杉醇。E7010是一种新型磺胺类药物,可抑制微管蛋白聚合。本文综述了这些药物的临床前和临床研究结果。