标记免疫分析与临床2024,Vol.31Issue(11) :2158-2168.DOI:10.11748/bjmy.issn.1006-1703.2024.11.034

锝(99Tcm)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 99Tcm Labeled Radiopharmaceuticals Targeting Fibroblast Activation Proteins

陈欢 黄旭虎
标记免疫分析与临床2024,Vol.31Issue(11) :2158-2168.DOI:10.11748/bjmy.issn.1006-1703.2024.11.034

锝(99Tcm)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 99Tcm Labeled Radiopharmaceuticals Targeting Fibroblast Activation Proteins

陈欢 1黄旭虎1
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作者信息

  • 1. 原子高科股份有限公司,北京 102413;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;中核集团放射性药物工程技术研究中心,北京 102413
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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(99Tcm)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99Tcm标记FAPI示踪剂逐渐受到关注.本综述对99Tcm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99Tcm-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.

Abstract

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,99Tcm labeled drugs also show promising advantages,such as simple preparation and wide application.Therefore,the technetium(99Tcm)labeled FAPI tracers used for SPECT imaging is gradually receiving more attentions.This review categorizes the molecular structures of technetium(99Tcm)labeled FAPI radiotracers,and analyzes the structure-activity relationship of the modified groups of linkers.Furthermore,the design strategies and research progress of the 99Tcm-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/99Tcm

Key words

Fibroblast activating protein/Radiopharmaceuticals/Structure-activity relationship/99Tcm

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出版年

2024
标记免疫分析与临床
中国同辐股份有限公司

标记免疫分析与临床

CSTPCD
影响因子:0.978
ISSN:1006-1703
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