Huang Rong, Pu Yu, Huang Shun, Yang Conghui, Yang Fake, Pu Yongzhu, Li Jindan, Chen Long, Huang Yunchao
Department of PET/CT Center, Yunnan Cancer Hospital, The Third Affiliated Hospital of Kunming Medical University, Cancer Center of Yunnan Province, Kunming, China.
Medical Imaging Key Laboratory of Sichuan Province, North Sichuan Medical College, Nanchong, China.
Front Oncol. 2022 May 25;12:854658. doi: 10.3389/fonc.2022.854658. eCollection 2022.
Fibroblast activation protein (FAP), a type II transmembrane serine protease, is highly expressed in more than 90% of epithelial tumors and is closely associated with various tumor invasion, metastasis, and prognosis. Using FAP as a target, various FAP inhibitors (FAPIs) have been developed, most of which have nanomolar levels of FAP affinity and high selectivity and are used for positron emission tomography (PET) imaging of different tumors. We have conducted a systematic review of the available data; summarized the biological principles of FAPIs for PET imaging, the synthesis model, and metabolic characteristics of the radiotracer; and compared the respective values of FAPIs and the current mainstream tracer F-Fludeoxyglucose (F-FDG) in the clinical management of tumor and non-tumor lesions. Available research evidence indicates that FAPIs are a molecular imaging tool complementary to F-FDG and are expected to be the new molecule of the century with better imaging effects than F-FDG in a variety of cancers, including gastrointestinal tumors, liver tumors, breast tumors, and nasopharyngeal carcinoma.
成纤维细胞活化蛋白(FAP)是一种II型跨膜丝氨酸蛋白酶,在90%以上的上皮性肿瘤中高表达,与各种肿瘤的侵袭、转移及预后密切相关。以FAP为靶点,已开发出多种FAP抑制剂(FAPI),其中大多数对FAP具有纳摩尔级亲和力且选择性高,用于不同肿瘤的正电子发射断层扫描(PET)成像。我们对现有数据进行了系统综述;总结了用于PET成像的FAPI的生物学原理、放射性示踪剂的合成模式及代谢特征;并比较了FAPI与当前主流示踪剂氟代脱氧葡萄糖(F-FDG)在肿瘤及非肿瘤病变临床管理中的各自价值。现有研究证据表明,FAPI是一种可补充F-FDG的分子成像工具,有望成为本世纪的新型分子,在包括胃肠道肿瘤、肝脏肿瘤、乳腺肿瘤及鼻咽癌在内的多种癌症中,其成像效果优于F-FDG。