Teaching and Research Division, School of Chinese Medicine, Hong Kong Baptist University, Kowloon, Hong Kong SAR, China.
Int J Mol Sci. 2021 Apr 12;22(8):3973. doi: 10.3390/ijms22083973.
Cyclopeptides or cyclic peptides are polypeptides formed by ring closing of terminal amino acids. A large number of natural cyclopeptides have been reported to be highly effective against different cancer cells, some of which are renowned for their clinical uses. Compared to linear peptides, cyclopeptides have absolute advantages of structural rigidity, biochemical stability, binding affinity as well as membrane permeability, which contribute greatly to their anticancer potency. Therefore, the discovery and development of natural cyclopeptides as anticancer agents remains attractive to academic researchers and pharmaceutical companies. Herein, we provide an overview of anticancer cyclopeptides that were discovered in the past 20 years. The present review mainly focuses on the anticancer efficacies, mechanisms of action and chemical structures of cyclopeptides with natural origins. Additionally, studies of the structure-activity relationship, total synthetic strategies as well as bioactivities of natural cyclopeptides are also included in this article. In conclusion, due to their characteristic structural features, natural cyclopeptides have great potential to be developed as anticancer agents. Indeed, they can also serve as excellent scaffolds for the synthesis of novel derivatives for combating cancerous pathologies.
环肽或环状肽是由末端氨基酸环化形成的多肽。大量的天然环肽已被报道对不同的癌细胞具有高度的有效性，其中一些因其临床用途而闻名。与线性肽相比，环肽在结构刚性、生化稳定性、结合亲和力和膜通透性方面具有绝对优势，这极大地促进了它们的抗癌效力。因此，发现和开发天然环肽作为抗癌药物仍然吸引着学术研究人员和制药公司。本文概述了过去 20 年发现的具有抗癌活性的环肽。本综述主要集中于具有天然来源的环肽的抗癌功效、作用机制和化学结构。此外，本文还包括对天然环肽的结构-活性关系、全合成策略以及生物活性的研究。总之，由于其特征结构特征，天然环肽具有作为抗癌药物开发的巨大潜力。事实上，它们也可以作为合成新型衍生物以对抗癌症病理的优异支架。
