LAUSR

Polypeptides are an important class of biodegradable polymers that have been widely used in drug delivery field. Owing to the controllable synthesis and robust side chain-functionalization ability, polypeptides have long been ideal candidates for conjugation with anticancer drugs. The chemical conjugation of anticancer drugs with polypeptides, termed polypeptides-drug conjugates, has demonstrated several advantages in improving pharmacokinetics, enhancing drug targeting, and controlling drug release, thereby leading to enhanced therapeutic outcomes with reduced side toxicities. This review focuses on the recent advances in the design and preparation of polypeptides-drug conjugates for enhanced anticancer therapy. Strategies for conjugation of different types of drugs, including small-molecule chemotherapeutic drugs, proteins, vascular disrupting agents, and gas molecules, onto polypeptides backbone are summarized. Finally, the challenges and future perspectives on the development of innovative polypeptides-drug conjugates for clinical cancer treatment are also presented.