Abstract: Integrin αvβ3 plays an essential role in tumor growth and metastasis, which is a target for cancer treatment. Integrin αvβ3 contains a variety of domains and its activation is very complicated. Among all the domains, β-propeller domain, βI domain and thigh domain are closely related to the activation of integrin αvβ3. In addition, varies of tumor-targeted drugs of integrin αvβ3 have been developed, including tumor imaging agents, agents for targeted therapeutic delivery and antitumor agents. This paper reviewed the relation between cancer and αvβ3, structure and activation of αvβ3, and tumor-targeted drugs of αvβ3, which provides theoretical basis for the future study of integrin αvβ3 and drug research.

Key words: integrin αvβ3, structure, activation, tumor, cancer, tumor-targeted drugs