Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives

被引：1

作者：

Yu, Ziyue ^{[1
]}

Jiang, Zeng ^{[1
]}

Cheng, Xuebo ^{[1
]}

Yuan, Leilei ^{[2
]}

Chen, Hualong ^{[1
]}

Ai, Lin ^{[2
]}

Wu, Zehui ^{[2
]}

机构：

[1] Capital Med Univ, Beijing Inst Brain Disorders, Collaborat Innovat Ctr Brain Disorders, Lab Brain Disorders,Minist Sci & Technol, Beijing 100069, Peoples R China

[2] Capital Med Univ, Beijing Tiantan Hosp, Dept Nucl Med, Beijing 100070, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2024年 / 277卷

基金：

北京市自然科学基金; 中国国家自然科学基金;

关键词：

Fibroblast activation protein-alpha; Radioligand; Radiopharmaceuticals; Positron emission tomography; Single-photon emission computed tomography; CANCER; INHIBITORS; TRACERS; DESIGN; FAP; PET;

D O I：

10.1016/j.ejmech.2024.116787

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Fibroblast activation protein-alpha (FAP) has emerged as a promising target in the field of radiopharmaceuticals due to its selective expression in cancer-associated fibroblasts (CAFs) and other pathological conditions involving fibrosis and inflammation. Recent advancements have focused on developing FAP-specific radioligands for diagnostic imaging and targeted radionuclide therapy. This perspective summarized the latest progress in FAP radiopharmaceutical development, highlighting novel radioligands, preclinical evaluations, and potential clinical applications. Additionally, we analyzed the advantages and existing problems of targeted FAP radiopharmaceuticals, and discussed the key breakthrough directions of this target, so as to improve the development and conversion of FAP-targeted radiopharmaceuticals.

引用

页数：52

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