Abstract: Abnormal protein-protein interaction(PPI) network is an important cause of tumors.Nowadays, a growing number of peptidederived materials have been widely and successfully used due to their unique advantages in the development of modulators targeting tumorrelated PPI regulators.Based on the design and application of peptides targeting PPI, this article summarizes related researches in recent years towards the development of anti-cancer drugs, in an attempt to provide historical reference for their future development.