放射性标记的 PARP-1 抑制剂在肿瘤中 PARP-1 表达成像中的应用现状及进展。

Current status and progress in using radiolabelled PARP-1 inhibitors for imaging PARP-1 expression in tumours.

机构信息

Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing, 100875, PR China.

出版信息

Eur J Med Chem. 2022 Nov 15;242:114690. doi: 10.1016/j.ejmech.2022.114690. Epub 2022 Aug 18.

DOI:10.1016/j.ejmech.2022.114690

PMID:36041258

Abstract

Poly(ADP-ribose) polymerase-1 (PARP-1) is a key enzyme in the DNA repair process, and the overexpression of PARP-1 in several tumours makes this enzyme a promising molecular target. Recently, several PARP-1 inhibitors, such as olaparib, rucaparib, niraparib and talazoparib, have been clinically approved as anticancer drugs. Several of these inhibitors have been radiolabelled for noninvasive imaging of PARP-1 expression in several types of tumours. In this review, the background and progress for using various radiolabelled PARP-1 inhibitors for cancer diagnosis are discussed and future development directions are proposed.

摘要

聚（ADP-核糖）聚合酶 1（PARP-1）是 DNA 修复过程中的关键酶，几种肿瘤中 PARP-1 的过表达使该酶成为有前途的分子靶点。最近，几种 PARP-1 抑制剂，如奥拉帕利、鲁卡帕利、尼拉帕利和他拉唑帕利，已被临床批准为抗癌药物。其中一些抑制剂已被放射性标记，用于几种类型肿瘤中 PARP-1 表达的无创成像。在这篇综述中，讨论了使用各种放射性标记的 PARP-1 抑制剂进行癌症诊断的背景和进展，并提出了未来的发展方向。