Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus P.O. Box 7, Palestine.
Biomolecules. 2022 Dec 10;12(12):1843. doi: 10.3390/biom12121843.
Cancer accounts for numerous deaths each year, and it is one of the most common causes of death worldwide, despite many breakthroughs in the discovery of novel anticancer candidates. Each new year the FDA approves the use of new drugs for cancer treatments. In the last years, the biological targets of anticancer agents have started to be clearer and one of these main targets is tubulin protein; this protein plays an essential role in cell division, as well as in intracellular transportation. The inhibition of microtubule formation by targeting tubulin protein induces cell death by apoptosis. In the last years, numerous novel structures were designed and synthesized to target tubulin, and this can be achieved by inhibiting the polymerization or depolymerization of the microtubules. In this review article, recent novel compounds that have antiproliferation activities against a panel of cancer cell lines that target tubulin are explored in detail. This review article emphasizes the recent developments of tubulin inhibitors, with insights into their antiproliferative and anti-tubulin activities. A full literature review shows that tubulin inhibitors are associated with properties in the inhibition of cancer cell line viability, inducing apoptosis, and good binding interaction with the colchicine binding site of tubulin. Furthermore, some drugs, such as cabazitaxel and fosbretabulin, have been approved by FDA in the last three years as tubulin inhibitors. The design and development of efficient tubulin inhibitors is progressively becoming a credible solution in treating many species of cancers.
癌症每年导致大量死亡，尽管在发现新的抗癌候选物方面取得了许多突破，但它仍是全球最常见的死因之一。每年，FDA 都会批准新的抗癌药物用于癌症治疗。近年来，抗癌药物的生物靶点开始变得更加清晰，其中一个主要靶点是微管蛋白；这种蛋白质在细胞分裂以及细胞内运输中起着至关重要的作用。通过靶向微管蛋白抑制微管形成会诱导细胞凋亡而导致细胞死亡。近年来，设计和合成了许多新型结构来靶向微管蛋白，这可以通过抑制微管的聚合或解聚来实现。在这篇综述文章中，详细探讨了最近针对微管蛋白具有增殖活性的新型化合物。本文综述强调了微管蛋白抑制剂的最新进展，深入了解其增殖抑制和抗微管蛋白活性。全面的文献综述表明，微管蛋白抑制剂与抑制癌细胞系活力、诱导细胞凋亡以及与微管蛋白的秋水仙碱结合位点良好结合的特性有关。此外，卡巴他赛和福司他丁等一些药物在过去三年中已被 FDA 批准为微管蛋白抑制剂。有效微管蛋白抑制剂的设计和开发正在逐渐成为治疗多种癌症的可靠方法。
