靶向PARP-1 PET/CT成像在肿瘤精准诊疗中应用研究进展  

Research progress on the application of targeted PARP-1 PET/CT imaging for cancer precision diagnosis and treatment

作　　者：唐嘉逸 华娜 许晨晨 张涛 韩雨霏[1,2] TANG Jia-yi;HUA Na;XU Chen-chen;ZHANG Tao;HAN Yu-fei(Department of Radiopharmaceuticals,School of Pharmacy,Nanjing Medical University,Nanjing 211166,China;Nuclear Medicine Clinical Transformation Center,Nanjing Medical University,Nanjing 210029,China;College of Nursing,Nanjing Medical University,Nanjing 211166,China)

机构地区：[1]南京医科大学药学院核药学系,江苏南京211166 [2]南京医科大学核医药临床转化中心,江苏南京210029 [3]南京医科大学护理学院,江苏南京211166

出　　处：《中国药物化学杂志》2023年第12期948-956,共9页Chinese Journal of Medicinal Chemistry

基　　金：江苏省高等学校大学生创新创业训练计划2022年立项项目:靶向PARP1 PET分子探针的构建项目(202210312075Y);国家自然科学基金项目(12275135);江苏省高校自然科学研究项目(21KJB350015);南京医科大学引进人才科研启动基金项目(NMUR20210003);南京医科大学内涵建设重点项目和南京医科大学科技发展基金项目(NMUB20210014);江苏省高校自然科学研究项目(22KJB350008)。

摘　　要：聚腺苷二磷酸核糖聚合酶1(PARP-1)是一种关键的DNA修复酶,具有DNA损伤应答、调控细胞凋亡、维持基因组稳定等作用,已成为当今肿瘤诊断与治疗的热门靶点。抑制PARP-1活性能够抑制肿瘤细胞DNA损伤修复,从而达到杀灭肿瘤细胞的目的。正电子发射断层成像(PET)通过使用放射性示踪剂在体内产生的正电子与体内其他电子发生相互作用,对活体组织器官代谢情况和微观病变进行分子水平的探测。在精准医学领域,PET通过直接测量药物靶点的表达水平或监测患者的治疗情况来识别早期反应,故具有早期诊断与鉴别肿瘤的潜力。近些年研究发现,放射性核素标记的PRAP-1 PET探针可以作为示踪剂,应用于肿瘤早期影像诊断、分期和疗效即时评估。本文综述了放射性核素标记的PARP-1靶向剂在精准诊疗中应用的研究进展,以期为新型靶向PARP-1 PET探针研发提供新思路与新方向。Poly ADP-ribose polymerase-1(PARP-1)is a key DNA repairing enzyme that plays the role of DNA damage response,regulation of cell apoptosis,maintenance of genomic stability,and has become a hot target for cancer diagnosis and treatment.The inhibition of PARP-1 activity can inhibit DNA damagerepairing in tumor cells,thereby achieving the purpose of killing tumor cells.Positron emission tomography(PET)uses a radioactive tracer to produce positron interactions with other electrons in the body,allowing molecular-level detection of metabolic conditions and micro-lesions in living tissue and organs.In precision medicine,PET can identify early responses by directly measuring the expression level of drug targets or monitoring patient treatment,making it potential for early diagnosis and differential diagnosis of tumors.In recent years,it has been found that radioactive nuclide-labeled PARP-1 PET probes can be used as tracers for early imaging diagnosis of tumors,staging and real-time evaluation of treatment efficacy.This paper reviewed the research progress on the application of targeted agents for radioactive nuclide-labeled PARP-1 in precision diagnosis and treatment,providing new ideas and directions for the development of new targeted PARP-1 PET probes.

关 键 词：癌症 PARP-1抑制剂 分子探针 PET 精准诊疗 

分 类 号：R914[医药卫生—药物化学]