酶促自组装分子在肿瘤治疗和成像中的研究进展  

Research progress of enzyme-instructed self-assembly molecules for tumor therapy and imaging

作　　者：任彦炜 李琦一 何冰[1] 李昊逾 赵丽 李玉艳[1] REN Yanwei;LI Qiyi;HE Bing;LI Haoyu;ZHAO Li;LI Yuyan(Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 211198;School of Basic Medicine and ClinicalPharmacology,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学药物化学系,南京211198 [2]中国药科大学基础医学与临床药学学院,南京211198

出　　处：《中国药科大学学报》2023年第4期431-442,共12页Journal of China Pharmaceutical University

基　　金：江苏省社会发展面上项目资助(No.BE20200695)。

摘　　要：自组装是生物大分子结构形成的基础方式之一。酶促自组装(enzyme-instructed self-assembly,EISA)借助工具酶,在特定的部位实现小分子化合物向超分子纳米结构的转换,成为药物开发的全新策略。近年来,EISA在恶性肿瘤的治疗和成像领域取得了长足的进步,实现了纳米结构的精确调控和肿瘤靶向。本文综述了EISA在肿瘤诊疗领域的最新进展,工具酶如碱性磷酸酶、去乙酰化酶、酪氨酸酶、γ-谷氨酰转肽酶和胱天蛋白酶3等的作用与特点,总结了在肿瘤治疗中EISA靶向多种细胞器的研究现状,并介绍了EISA在肿瘤成像中的运用,为EISA策略在肿瘤诊疗中的应用研究提供参考。Self-assembly is the basis of the formation of biological macromolecular structure.Enzyme-instructed self-assembly(EISA)with the help of tool enzymes,realizing the conversion of small molecular compounds to supramolecular nanostructures at specific sites,become a new strategy for drug discovery.In recent years,the exploration of EISA for developing malignant cancer therapy and imaging has made considerable progress,achieving the precise regulation and tumor targeting of nanostructures.This paper reviews the latest progress of EISA in the field of tumor diagnosis and treatment,the functions and characteristics of tool enzymes such as alka⁃line phosphatase,sirtuin,tyrosinase,γ-glutamyltranspeptidase and caspase-3,summarizes the research status of EISA targeting multiple organelles in tumor therapy,and introduces the application of EISA in tumor imaging,aiming to provide reference forthe research of EISA strategy in tumor diagnosis and treatment.

关 键 词：酶促自组装 细胞器靶向 分子成像 肿瘤 进展 

分 类 号：R318[医药卫生—生物医学工程]