Anti-cancer peptides (ACPs) are a series of short peptides composed of 10–60 amino acids that can inhibit tumour cell proliferation or migration, or suppress the formation of tumour blood vessels, and are less likely to cause drug resistance. The aforementioned merits make ACPs the most promising anti-cancer candidate. However, ACPs may be degraded by proteases, or result in cytotoxicity in many cases. To overcome these drawbacks, a plethora of research has focused on reconstruction or modification of ACPs to improve their anti-cancer activity, while reducing their cytotoxicity. The modification of ACPs mainly includes main chain reconstruction and side chain modification. After summarizing the classification and mechanism of action of ACPs, this paper focuses on recent development and progress about their reconstruction and modification. The information collected here may provide some ideas for further research on ACPs, in particular their modification.

抗癌肽（ACPs）是由10-60个氨基酸组成的一系列短肽，可以抑制肿瘤细胞增殖或迁移，或抑制肿瘤血管的形成，不易引起耐药性。上述优点使 ACP 成为最有前途的抗癌候选药物。然而，ACP 可能会被蛋白酶降解，或在许多情况下导致细胞毒性。为了克服这些缺点，大量的研究集中在 ACP 的重建或修饰上，以提高其抗癌活性，同时降低其细胞毒性。ACPs的修饰主要包括主链重构和侧链修饰。本文在总结了ACPs的分类和作用机制的基础上，重点介绍了ACPs重建和修饰的最新发展和进展。