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At present,the development of antineoplastic drugs has been highly concerned.Many strategies have been developed to explore the safety and effectiveness of antitumor drugs.In recent years,the progress of structural analysis of tumor-associated proteins provides a solid foundation for the design of new targeted drugs through efficient prediction and screening technology.In this review,we briefly summarize the research and development of new antitumor drugs based on structure to enhance tumor targeting property and reduce side effects.