靶向成纤维细胞活化蛋白PET显像剂的研究进展

Research progress of PET imaging agents targeting fibroblast activation protein

成纤维细胞活化蛋白(FAP)在90%上皮肿瘤的肿瘤相关成纤维细胞中过表达,而在正常组织中几乎不表达,因此FAP是肿瘤诊疗的重要靶标。一系列靶向FAP的显像剂在临床前研究PET显像中展现出良好的成像结果,其表现为特异性高摄取和非靶向性低摄取。与氟脱氧葡萄糖显像相比,FAP显像在大多数恶性肿瘤中显示出更高的摄取值和灵敏性。大量的临床研究也逐步开展。靶向FAP的显像剂在多种恶性肿瘤的研究中取得了一定的进展,且有研究证实FAP在部分非肿瘤性疾病(如心肌梗死、免疫球蛋白G亚型4、结核等)中也会有高表达,因此靶向FAP的显像剂也可用于非肿瘤性疾病的诊断。笔者就靶向FAP的PET新型分子探针及其临床转化的研究进展进行综述。

Fibroblast activation protein(FAP)is overexpressed in cancer-associated fibroblasts in 90%of epithelial tumors,but hardly expressed in normal tissues.Therefore,FAP is an important target for tumor diagnosis and treatment.A series of imaging agents targeting FAP have shown favorable imaging results in preclinical studies with specific high uptake and non-targeted low uptake.Compared with fluorodeoxyglucose imaging,FAP imaging showed higher uptake value and sensitivity in most malignancies.Since then,a large number of clinical studies have been gradually carried out.Some progress has been made in the study of various malignant tumors with imaging agents targeting FAP,and some studies have confirmed that FAP is effective in some non-tumor diseases(such as myocardial infarction,immunoglobulin G4,Tuberculosis,etc.)are also highly expressed.So imaging agents targeting FAP can also be used for the diagnosis of non-neoplastic diseases.This article reviews the research progress of novel molecular probes for PET targeting FAP and their clinical translation.