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AZD1390,一种共济失调毛细血管扩张症突变抑制剂,可增强顺铂介导的乳腺癌细胞凋亡。

AZD1390, an Ataxia telangiectasia mutated inhibitor, enhances cisplatin mediated apoptosis in breast cancer cells.

作者信息

Özdemir Deniz, Ağca Can Ali

机构信息

Bingöl University, Faculty of Arts and Sciences, Department of Molecular Biology and Genetics, 12000, Bingöl, Türkiye.

出版信息

Exp Cell Res. 2025 Jan 15;444(2):114382. doi: 10.1016/j.yexcr.2024.114382. Epub 2024 Dec 15.

Abstract

Genomic instability is often caused by deficiencies in DNA damage repair pathways, making therapeutic targeting of DDR beneficial for cancer patients with specific DDR functions. ATM kinase plays a critical role in various cellular processes and its deficiency increases sensitivity to DDR-targeted agents in different cancers. Recent studies highlight ATM inhibition as a potential clinical target, with AZD1390 being a notable ATM inhibitor due to its potent and selective inhibition, ability to accumulate at DNA breaks. The study aimed to evaluate the potential anti-cancer effects of AZD1390, a key component of the DNA damage response, in breast cancer cells. The impact of the combination of AZD1390 and cisplatin on various parameters such as cell viability, proliferation, colony formation capacity, DNA damage, reactive oxygen species (ROS) levels, mitochondrial membrane potential, cell cycle progression, and cell death in breast cancer cells was evaluated using several methodologies, including WST-1 assays, real-time cell analysis, colony formation assays, comet assays, DCF-DA, MMP/JC-1 staining assays, flow cytometry along with Western blot analysis. We found that AZD1390 and cisplatin displayed synergistic antitumor effects in breast cancer cells at low doses. Addinationaly exhibited significant anti-proliferative effects in colony formation and real-time cell proliferation experiments, increasing intracellular ROS levels and mitochondrial membrane potential.The combined treatment also arrested the cell cycle at the G2-M point. Furthermore, combination of AZD1390 with cisplatin enhances its apoptotic effects in MCF-7 and MDA-MB-231 cells. These findings could aid in developing new treatments for breast cancer that exploit the genomic instability of cancer cells.

摘要

基因组不稳定通常由DNA损伤修复途径的缺陷引起,这使得针对DDR功能的治疗性靶向对具有特定DDR功能的癌症患者有益。ATM激酶在各种细胞过程中起关键作用,其缺陷会增加不同癌症对DDR靶向药物的敏感性。最近的研究强调ATM抑制作为一种潜在的临床靶点,AZD1390因其强效和选择性抑制以及在DNA断裂处积累的能力而成为一种显著的ATM抑制剂。该研究旨在评估DNA损伤反应的关键成分AZD1390在乳腺癌细胞中的潜在抗癌作用。使用多种方法,包括WST-1测定、实时细胞分析、集落形成测定、彗星试验、DCF-DA、MMP/JC-1染色测定、流式细胞术以及蛋白质印迹分析,评估了AZD1390和顺铂联合对乳腺癌细胞中各种参数的影响,如细胞活力、增殖、集落形成能力、DNA损伤、活性氧(ROS)水平、线粒体膜电位、细胞周期进程和细胞死亡。我们发现AZD1390和顺铂在低剂量时对乳腺癌细胞显示出协同抗肿瘤作用。此外,在集落形成和实时细胞增殖实验中还表现出显著的抗增殖作用,增加细胞内ROS水平和线粒体膜电位。联合治疗还使细胞周期停滞在G2-M期。此外,AZD1390与顺铂联合增强了其在MCF-7和MDA-MB-231细胞中的凋亡作用。这些发现有助于开发利用癌细胞基因组不稳定的乳腺癌新疗法。

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