Abstract
The dual challenges of drug resistance and toxicity in cancer therapy necessitate the development of new drugs with high efficacy and safety. Selenopeptides, which synergistically combine selenium's redox regulation capabilities with the tumor-targeting specificity of peptides, represent a promising frontier in antitumor drug development. Based on the recent literature, this review summarizes the sources and preparation methods of selenium peptides, such as enzymatic hydrolysis and solid/liquid-phase synthesis. Furthermore, it elucidates their multitarget mechanisms of action, including the modulation of the PI3K/Akt signaling pathway, activation of immune cells, inhibition of angiogenesis, and induction of cancer cell apoptosis. Evidence from in vitro, in vivo and preliminary clinical studies confirms their effectiveness in inhibiting cancer cell proliferation and reducing tumor markers. This article reviews the current research progress to provide a comprehensive reference for the clinical translation and application of selenium peptides in cancer therapy.