核素标记聚腺苷二磷酸核糖聚合酶抑制剂显像剂研究进展

The Progress of Radionuclide-labeled Poly Adenosine DiphosphateRibose Polymerase Imaging Agent

聚腺苷二磷酸核糖聚合酶(PARP)是一种DNA修复酶,参与基因转录、炎症、凋亡、细胞死亡和代谢等生命过程。在增殖活跃的细胞中PARP表达和活性增加,特别是在多种癌细胞中过度表达。聚腺苷二磷酸核糖聚合酶抑制剂(PARPi)可以治疗卵巢癌、乳腺癌、前列腺癌、输卵管癌、腹膜癌、胰腺癌等恶性肿瘤。通过放射性核素对PARPi类似物进行标记,靶向结合PARP-1,构建放射性显像剂进行肿瘤显像,可用于治疗决策和疗效评估等。本文将总结核素标记聚腺苷二磷酸核糖聚合酶显像剂的研究进展。

Poly adenosine diphosphate ribose polymerase(PARP)is a DNA repair enzyme involved in various life processes,such as gene transcription,inflammation,apoptosis,cell death,and metabolism.PARP are expressed in proliferating cells,especially in a variety of cancer cells.Poly adenosine diphosphate ribose polymerase inhibitors(PARPi)can be used in the treatment of malignant tumors,such as ovarian cancer,breast cancer,prostate cancer,fallopian tube cancer,peritoneal cancer,and pancreatic cancer,etc.By labeling PARPi analogues with radionuclides and targeting PARP-1,these constructed radionuclide imaging agents can be used for tumor imaging and treatment decision-making and efficacy evaluation.This article summarizes the current research progress of radionuclide-labeled poly adenosine diphosphate ribose polymerase imaging agents.