Department of Drug Chemistry and Technologies, Sapienza University of Rome, Laboratory affiliated to Istituto Pasteur Italia - Fondazione Cenci Bolognetti, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
Department of Drug Chemistry and Technologies, Sapienza University of Rome, Laboratory affiliated to Istituto Pasteur Italia - Fondazione Cenci Bolognetti, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
Eur J Pharm Sci. 2019 Apr 1;131:58-68. doi: 10.1016/j.ejps.2019.01.028. Epub 2019 Jan 25.
Tubulin is the primary target of an ever growing number of natural, semisynthetic and synthetic products as potential anticancer agents. The mechanisms of interaction of these molecules with tubulin are varied. These drug classes have shown to inhibit effectively several cancer types with IC from midmicromolar to low nanomolar concentrations. However, some limiting obstacles still remain, such as the development of multidrug resistance and cytotoxicity. We have reviewed recent advances in different classes of tubulin binding agents, including colchicine site agents, Vinca alkaloids, tryprostatins, moroidin, hemiasterlin, diazonamide, taxanes, epothilones and laulimalide.
微管蛋白是越来越多天然、半合成和合成产物作为潜在抗癌剂的主要靶点。这些分子与微管蛋白相互作用的机制多种多样。这些药物类别已被证明能有效地抑制多种癌症类型，IC50 从中等微摩尔到低纳摩尔浓度。然而，仍然存在一些限制因素，如多药耐药性和细胞毒性的发展。我们综述了不同类型的微管蛋白结合剂的最新进展，包括秋水仙碱结合剂、长春花生物碱、三普瑞他汀、莫罗定、海兔毒素、重氮酰胺、紫杉烷类、埃坡霉素和拉罗他赛。
