成纤维细胞激活蛋白靶向药物及其用于疾病显像和治疗的研究进展  

Research progress of fibroblast activation protein targeting drugs and their application in disease imaging and therapy

作　　者：吴丹丹[1] 邵国强[2] 孔霞[1] 张莉[1] Wu Dandan;Shao Guoqiang;Kong Xia;Zhang Li(Department of Pediatrics,Nanjing First Hospital,Nanjing Medical University,Nanjing 210006,China;Department of Nuclear Medicine,Nanjing First Hospital,Nanjing Medical University,Nanjing 210006,China)

机构地区：[1]南京医科大学附属南京医院(南京市第一医院)儿科,南京210006 [2]南京医科大学附属南京医院(南京市第一医院)核医学科,南京210006

出　　处：《国际放射医学核医学杂志》2023年第1期45-51,共7页International Journal of Radiation Medicine and Nuclear Medicine

基　　金：江苏省高层次卫生人才"六个一工程"拔尖人才科研项目(LGY2019005);江苏省"科教强卫工程"青年医学人才(QNRC2016075);南京市卫生科技发展专项资金(医学重点科技发展项目)(ZKX19022)。

摘　　要：成纤维细胞激活蛋白(FAP)在90%以上的上皮性肿瘤的癌症相关成纤维细胞(CAFs)中高丰度表达,具有特异性和广谱性,是肿瘤微环境靶向显像和治疗的研究热点。FAP靶向抗体、小分子抑制剂和多肽作为配体,通过偶联核素以及荧光探针用于肿瘤靶向显像、治疗、精准手术导航,并通过二聚体化以及新剂型构建(如白蛋白、纳米递送系统等)优化FAP靶向药物的生物分布,进而增加其在肿瘤内的滞留时间和增强生物学作用,推动其用于肿瘤靶向内放射性治疗和光热治疗。除了肿瘤,FAP也可为炎性疾病的显像和治疗提供有价值的靶点。笔者就近年来FAP在肿瘤和非肿瘤性疾病中的显像和治疗的研究进展进行综述。Fibroblast activation protein(FAP)is highly expressed in cancer-associated fibroblasts(CAFs)of more than 90%epithelial tumors with specificity and broad spectrum.FAP ligands,such as targeted antibodies,small molecule inhibitors and peptides,are used in tumor targeted imaging,therapy and precise surgical navigation by coupling radionuclides and fluorescent probes.Moreover,through dimerization,construction of new dosage forms such as albumin,nano-delivery system and other means to optimize the biological distribution of FAP targeted drug to increase its retention and biological effects in tumor and promote its use in tumor targeted internal radiation therapy and photothermal therapy.In addition to neoplastic diseases,FAP can also provide valuable targets for imaging and therapy of inflammatory disease.This article reviews the research progress of imaging and therapy of FAP in tumor and non-tumor diseases in recent years.

关 键 词：成纤维细胞 放射疗法 放射性同位素 靶向制剂 成纤维细胞激活蛋白 

分 类 号：R914[医药卫生—药物化学]