靶向脑内异常蛋白聚集体的PET显像剂研究进展  

Research Progress of PET Imaging Agents Targeting Abnormal Protein Aggregates in the Brain

作　　者：郭万通 李钰莹 崔孟超[1] GUO Wantong;LI Yuying;CUI Mengchao(Key Laboratory of Radiopharmaceuticals(Beijing Normal University),Ministry of Education,Beijing 100875,China)

机构地区：[1]北京师范大学放射性药物教育部重点实验室,北京100875

出　　处：《药学进展》2024年第3期166-177,共12页Progress in Pharmaceutical Sciences

摘　　要：大多数神经退行性疾病被证实与脑内特定蛋白质的错误折叠与异常聚集有关,如β-淀粉样蛋白斑块和Tau蛋白的异常聚集是阿尔茨海默病的两个重要病理学特征,α-突触核蛋白聚集体是帕金森病和路易体痴呆的生物学标志物,突变亨廷顿蛋白是亨廷顿舞蹈症的生物学标志物。在过去的几十年里,随着正电子发射断层扫描(PET)技术和放射性诊断药物的发展,PET显像被越来越多地应用于中枢神经系统疾病的早期诊断和相关治疗药物的疗效评估。综述了靶向于上述4种蛋白聚集体的PET显像剂的研究进展,为相关PET显像剂的进一步结构优化与临床应用提供思路与参考。Most neurodegenerative diseases(NDDs)have been shown to be associated with the misfolding and abnormal aggregation of specific proteins in the brain.For example,abnormal aggregation of amyloidβ-protein(Aβ)plaques and Tau protein are two important pathological features of Alzheimer's disease(AD).α-Synuclein(α-Syn)aggregates are biological markers of Parkinson's disease(PD)and dementia with Lewy body(DLB),while mutated huntingtins(mHTTs)serve as biological markers for Huntington's disease(HD).In the past few decades,positron emission tomography(PET)and diagnostic radiopharmaceuticals have been developed,leading to an increase in the use of PET imaging for early diagnosis of central nervous system diseases and the evaluation of related therapeutic drugs.In this article,the research progress of PET imaging agents targeting the above four types of protein aggregates was reviewed,aiming to provide ideas and references for further structural optimization and clinical application of related PET imaging agents.

关 键 词：正电子发射断层扫描 显像剂 蛋白聚集体 阿尔茨海默病 帕金森病 亨廷顿舞蹈症 

分 类 号：R817.9[医药卫生—影像医学与核医学]