Abstract:The incidence of cancer is increasing year by year, and malignant tumors seriously affect human health and life. At present, conventional anticancer drugs are losing some therapeutic applications due to their low targeting, obvious toxic and side effects, and drug resistance. The anti-tumor polypeptide drugs have the characteristics of small molecular weight, high specificity, weak toxicity, easy synthesis and so on, which makes them become a new drug for treatment of tumor. Antitumor peptides mainly include natural peptides, artificial modified peptides and synthetic peptides. Its mechanism of anti-tumor is very complex, including inhibition of tumor cell proliferation, migration and invasion, promotion of tumor cell apoptosis and immunoregulation. In this review, an overview of anti-tumor peptides based on blocking protein-protein interactions will be presented.