整合素αvβ3结构与激活及其肿瘤靶向药物的研究进展

Research progress in structure,activation and tumor-targeted drugs of integrin αvβ3

整合素αvβ3在肿瘤生长及转移过程中发挥重要作用,是一个治疗癌症的靶点。整合素αvβ3结构域众多,激活过程非常复杂,其中激活关键的结构域有β-propeller结构域、βI结构域以及thigh结构域。此外,针对αvβ3已经开发出很多肿瘤相关靶向药物,如肿瘤显影药、靶向运输治疗药以及直接抗肿瘤药。就整合素αvβ3与癌症、结构与激活以及αvβ3肿瘤相关靶向药物这几方面进行综述,为进一步研究整合素αvβ3的结构功能以及药物提供了一定理论基础。

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.