School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China; Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Bioorg Med Chem Lett. 2021 Apr 1;37:127698. doi: 10.1016/j.bmcl.2020.127698. Epub 2021 Jan 16.
Tubulin, an important target in tumor therapy, is one of the hotspots in the field of antineoplastic drugs in recent years, and it is of great significance to design and screen new inhibitors for this target. Natural products and chemical synthetic drugs are the main sources of tubulin inhibitors. However, due to the variety of compound structure types, it has always been difficult for researchers to screen out polymerization inhibitors with simple operation, high efficiency and low cost. A large number of articles have reported the screening methods of tubulin inhibitors and their biological activity. In this article, the biological activity detection methods of tubulin polymerization inhibitors are reviewed. Thus, it provides a theoretical basis for the further study of tubulin polymerization inhibitors and the selection of methods for tubulin inhibitors.
微管蛋白是肿瘤治疗的重要靶点之一,也是近年来抗肿瘤药物领域的热点之一,设计和筛选针对该靶点的新型抑制剂具有重要意义。天然产物和化学合成药物是微管蛋白抑制剂的主要来源。然而,由于化合物结构类型的多样性,研究人员一直难以筛选出操作简单、高效、低成本的聚合抑制剂。大量文献报道了微管蛋白抑制剂的筛选方法及其生物活性。本文综述了微管蛋白聚合抑制剂的生物活性检测方法,为进一步研究微管蛋白聚合抑制剂及其方法选择提供了理论依据。