药学学报, 2010, 45(9): 1078-1088
引用本文:
尚 海 潘 莉 杨 澍 陈 虹 程卯生. 微管蛋白抑制剂的研究进展[J]. 药学学报, 2010, 45(9): 1078-1088.
CHANG Hai, Bo- Chi, Yang- Shu, Chen- Gong, Cheng-Mao-Sheng. Progress in the study of tubulin inhibitors[J]. Acta Pharmaceutica Sinica, 2010, 45(9): 1078-1088.

微管蛋白抑制剂的研究进展
尚 海1, 潘 莉1, 杨 澍1, 陈 虹2, 程卯生1*
(1. 沈阳药科大学制药工程学院, 基于靶点的药物设计与研究教育部重点实验室, 辽宁 沈阳 110016; 2. 中国人民武装警察部队医学院, 天津 300162)
摘要:

微管是细胞骨架的主要组成部分, 在维持细胞形态、细胞分裂、信号转导等过程中起着重要作用。由于微管在细胞分裂过程中的重要作用, 微管蛋白已经成为研究与开发全新抗癌药物的要靶点之一, 作用于微管系统的微管蛋白抑制剂也已成为一类有效的抗肿瘤药物。该类抑制剂的作用机制是通过抑制微管蛋白的聚合或者促进微管蛋白的聚合而干扰细胞的有丝分裂过程, 从而发挥抗肿瘤作用。本文对近年来微管蛋白抑制剂的研究进展进行了总结, 着重介绍了微管蛋白抑制剂的药理活性和临床研究进展, 并探讨了该类抑制剂的发展趋势。

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Progress in the study of tubulin inhibitors
Abstract:

Microtubule is one of the key components of the cytoskeleton and plays an important role in the maintenance of cell shape and the process of signal transduction and mitosis.  Due to the extreme importance  of microtubule in the process of mitosis, tubulin becomes one of the most important targets for development of new anticancer drugs and tubulin inhibitors are used for the treatment of cancer nowadays.  These inhibitors have antitumor activity by inhibiting or promoting the assembly of tubulin to microtubules and interfering the process of cell mitosis.  This review summarized the research progress of the tublulin inhibitors, especially the introduction of the tubulin inhibitors of pharmacological activities and the progress of clinical research.  Also, the development trend of these inhibitors is discussed.

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