锝(^(99)Tc^(m))标记的靶向成纤维细胞活化蛋白放射性药物研究进展  

The Research Progress of ^(99)Tc^(m)Labeled RadiopharmaceuticalsTargeting Fibroblast Activation Proteins

作　　者：陈欢 黄旭虎 CHEN Huan;HUANG Xuhu(HTA Co.,Ltd.,Beijing 102413,China;CAEA Center of Excellence on Nuclear Technology Applications forEngineering and Industrialization of Radiopharmaceuticals,Beijing 102413,China;CNNC EngineeringResearch Center of Radiopharmaceuticals,Beijing 102413,China)

机构地区：[1]原子高科股份有限公司,北京102413 [2]国家原子能机构核技术(放射性药物工程转化)研发中心,北京102413 [3]中核集团放射性药物工程技术研究中心,北京102413

出　　处：《标记免疫分析与临床》2024年第11期2158-2168,共11页Labeled Immunoassays and Clinical Medicine

摘　　要：成纤维细胞活化蛋白(FAP)存在于肿瘤基质成纤维细胞表面,是近年来肿瘤显像的重要靶点。虽然FAP靶向正电子药物发展迅速,但是锝(^(99)Tc^(m))标记药物具有制备简单、应用广泛等优点,因此,应用于单光子发射计算机断层扫描(SPECT)的^(99)Tc^(m)标记FAPI示踪剂逐渐受到关注。本综述对^(99)Tc^(m)标记FAPI药物分子结构进行分类和梳理,分析了连接部分修饰基团的构效关系。此外,着重介绍了^(99)Tc^(m)-FAPI示踪剂设计策略和研发进展,并对其进行总结和展望,为未来FAPI类SPECT/CT放射性药物研发与转化梳理方向。Fibroblast activation protein(FAP),which is present on the surface of cancer associated fibroblasts,has recently become an important target for tumor imaging.Although FAP targeted positron radiopharmaceuticals have developed rapidly,^(99)Tc^(m)labeled drugs also show promising advantages,such as simple preparation and wide application.Therefore,the technetium(^(99)Tc^(m))labeled FAPI tracers used for SPECT imaging is gradually receiving more attentions.This review categorizes the molecular structures of technetium(^(99)Tc^(m))labeled FAPI radiotracers,and analyzes the structure-activity relationship of the modified groups of linkers.Furthermore,the design strategies and research progress of the ^(99)Tc^(m)-FAPI tracers are emphasized.A systematic summary and outlook is provided to guide the future development and transformation of FAPI-based radiopharmaceuticals for SPECT/CT imaging.

关 键 词：成纤维细胞活化蛋白 放射性药物 构效关系 ^(99)Tc^(m) 

分 类 号：R817-3[医药卫生—影像医学与核医学]