Taipei Medical University, School of Pharmacy, College of Pharmacy , 250 Wuxing Street, Taipei 11031, Taiwan , Republic of China +886 2 2736 1661, ext 6130 ;
Expert Opin Ther Pat. 2014 Jan;24(1):69-88. doi: 10.1517/13543776.2014.859247. Epub 2013 Dec 9.
Microtubules play an important role in several cellular processes, particularly in the formation of the mitotic spindle during the process of mitosis. These highly dynamic mitotic-spindle microtubules have become a successful target of cancer therapy. Microtubule-targeting agents, such as vinca alkaloids and taxanes, were used in clinic over 50 years. In past decades, development of new antimicrotubule agents that possess different structure and binding sites of tubulin has shown potent activity against the proliferation of various cancer cells, as well as in multidrug-resistant cancers. Interestingly, many of these agents represent an attractive ability that targeting the tumor blood vessels results in tumor vascular disruption. Therefore, exploring new agents and strategies may provide more effective therapeutic options in the related treatment of cancer.
In past few years, there are many chemical compounds that successfully interferes the microtubules and display antitumor effect. In these, published compounds supply the fresh minds in modification of present drugs and new insights into the development of tubulin inhibitors.
This article arranges the microtubule-targeting agents that have published in patent in recent years. It may help in the investigation of new tubulin binding site and development of novel drug candidate in the future.
微管在多个细胞过程中发挥着重要作用，特别是在有丝分裂过程中形成有丝分裂纺锤体的过程中。这些高度动态的有丝分裂纺锤体微管已成为癌症治疗的成功靶点。微管靶向药物，如长春花生物碱和紫杉烷，已经在临床上使用了 50 多年。在过去的几十年中，开发具有不同结构和微管结合位点的新型抗微管药物，对各种癌细胞的增殖以及多药耐药性癌症表现出了强大的活性。有趣的是，其中许多药物具有靶向肿瘤血管的作用，导致肿瘤血管破裂，这是一种有吸引力的能力。因此，探索新的药物和策略可能为癌症的相关治疗提供更有效的治疗选择。
在过去的几年中，有许多化学化合物成功地干扰微管并显示出抗肿瘤作用。其中，已发表的化合物为现有药物的修饰和微管抑制剂的开发提供了新的思路。
本文整理了近年来在专利中发表的微管靶向药物。它可能有助于未来对新的微管结合位点的研究和新型药物候选物的开发。
