首页|放射性标记小分子抑制剂用作靶向FAP肿瘤显像剂的现状与展望

放射性标记小分子抑制剂用作靶向FAP肿瘤显像剂的现状与展望

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成纤维细胞活化蛋白(FAP)存在于肿瘤基质成纤维细胞中,是近年来肿瘤诊断和治疗的一个重要靶点。在靶向FAP的放射性肿瘤显像剂中,小分子类显像剂受到了最广泛的关注。本文介绍了靶向FAP小分子显像剂的核心结构,并对 2023年 12月前新型FAP小分子显像剂的设计策略进行分类。此外,对目前表现优良或具有新颖结构的靶向FAP的PET显像剂和SPECT显像剂进行了系统梳理,并对其结构和设计思路进行总结和展望,以期对临床诊疗有所助益。
Status and Prospect of Radiolabeled Small Molecule Inhibitors as Tumor Imaging Agents Targeting FAP
Fibroblast activation protein(FAP)exists in tumor stromal fibroblasts and is a significant target for tumor diagnosis and treatment recently.Among the radioactive FAP-targeted tumor imaging agents,small-molecule tracers have received the most extensive attention.This paper elucidates the core structure of FAP-targeted small molecule drugs,categorizes the various design approaches employed for the development of novel small molecule imaging agents targeting FAP,up until December 2023.Additionally,a comprehensive analysis of FAP-targeted PET imaging agents and SPECT imaging agents with excellent biological performance or innovative structure is conducted.The structures and design concepts of these agents are carefully examined and summarized,with the aim of making valuable contributions to clinical diagnosis and treatment.

FAPsmall molecule drugtumor imaging agent

韩沛雯、阮晴、张俊波

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北京师范大学化学学院,放射性药物教育部重点实验室,国家药监局放射性药物研究与评价重点实验室,北京 100875

射线束技术教育部重点实验室,北京师范大学核科学与技术学院,北京 100875

FAP 小分子药物 放射性肿瘤显像剂

国家自然科学基金国家自然科学基金北京市自然科学基金中国博士后科学基金北京市科技新星计划交叉学科合作项目

220760132227601522320102022M72046420230484470

2024

同位素
中国核学会同位素分会

同位素

CSTPCD
影响因子:0.405
ISSN:1000-7512
年,卷(期):2024.37(2)
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