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

Status and Prospect of Radiolabeled Small Molecule Inhibitors as Tumor Imaging Agents Targeting FAP

  • 摘要: 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。

     

    Abstract: 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.

     

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