摘要
多腺苷二磷酸核糖聚合酶(PARP)是广泛存在于真核生物细胞核内的一系列具有多功能的酶,在修复损伤DNA、衰老、染色质重塑和转录方面有重要作用。其中PARP-1在肿瘤细胞中过度表达,是DNA损伤修复中的关键作用因子。PARP抑制剂(PARPi)通过与PARP-1的催化位点结合并抑制其活性,从而阻碍肿瘤细胞DNA复制和损伤修复,起到治疗肿瘤的作用,但PARPi的肿瘤治疗效果直接与肿瘤PARP的表达相关。该文对基于PARP靶点的PET显像剂与治疗性放射性药物的研发现状、存在问题及其临床应用前景进行综述。
Poly(adenosine diphosphate-ribose)polymerase(PARP)is a series of enzymes with multiple functions widely present in the nuclei of eukaryotic cells,playing a crucial role in DNA damage repair,senility,chromatin remodeling,and transcriptional regulation.Notably,PARP-1 is overexpressed in tumor cells and serves as a pivotal factor in DNA damage repair.PARP inhibitors(PARPi)bind to the catalytic site of PARP-1,thereby inhibiting its activity and impeding DNA replication and repair in tumor cells,leading to therapeutic effects.However,the efficacy of PARPi is directly correlated with PARP expression levels in tumors.This review summarizes the current research and development status,existing challenges,and clinical application prospects of PET imaging agents and therapeutic radiopharmaceuticals targeting the PARP pathway.
作者
向鸿
王云华
Xiang Hong;Wang Yunhua(Department of Nuclear Medicine&PET Imaging Center,the Second Xiangya Hospital,Central South University,Changsha 410011,China)
出处
《中华核医学与分子影像杂志》
北大核心
2025年第12期760-764,共5页
Chinese Journal of Nuclear Medicine and Molecular Imaging
