Nie Litong, Wang Chao, Huang Min, Liu Xiaoguang, Feng Xu, Tang Mengfan, Li Siting, Hang Qinglei, Teng Hongqi, Shen Xi, Ma Li, Gan Boyi, Chen Junjie
Department of Experimental Radiation Oncology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.
Institute for Personalized Cancer Therapy, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.
bioRxiv. 2024 Feb 2:2023.07.31.551317. doi: 10.1101/2023.07.31.551317.
Poly(ADP-ribose)ylation or PARylation by PAR polymerase 1 (PARP1) and dePARylation by poly(ADP-ribose) glycohydrolase (PARG) are equally important for the dynamic regulation of DNA damage response. PARG, the most active dePARylation enzyme, is recruited to sites of DNA damage via pADPr-dependent and PCNA-dependent mechanisms. Targeting dePARylation is considered an alternative strategy to overcome PARP inhibitor resistance. However, precisely how dePARylation functions in normal unperturbed cells remains elusive. To address this challenge, we conducted multiple CRISPR screens and revealed that dePARylation of S phase pADPr by PARG is essential for cell viability. Loss of dePARylation activity initially induced S phase-specific pADPr signaling, which resulted from unligated Okazaki fragments and eventually led to uncontrolled pADPr accumulation and PARP1/2-dependent cytotoxicity. Moreover, we demonstrated that proteins involved in Okazaki fragment ligation and/or base excision repair regulate pADPr signaling and cell death induced by PARG inhibition. In addition, we determined that PARG expression is critical for cellular sensitivity to PARG inhibition. Additionally, we revealed that PARG is essential for cell survival by suppressing pADPr. Collectively, our data not only identify an essential role for PARG in normal proliferating cells but also provide a potential biomarker for the further development of PARG inhibitors in cancer therapy.
聚(ADP-核糖)聚合酶1(PARP1)介导的聚(ADP-核糖)基化作用(PARylation)以及聚(ADP-核糖)糖苷水解酶(PARG)介导的去聚(ADP-核糖)基化作用(dePARylation)对于DNA损伤反应的动态调节同样重要。PARG是活性最强的去聚(ADP-核糖)基化酶,可通过依赖于聚(ADP-核糖)磷酸酯(pADPr)和增殖细胞核抗原(PCNA)的机制被招募至DNA损伤位点。靶向去聚(ADP-核糖)基化作用被认为是克服PARP抑制剂耐药性的一种替代策略。然而,去聚(ADP-核糖)基化作用在正常未受干扰的细胞中的确切作用机制仍不清楚。为应对这一挑战,我们进行了多项CRISPR筛选,并发现PARG对S期pADPr的去聚(ADP-核糖)基化作用对于细胞活力至关重要。去聚(ADP-核糖)基化活性的丧失最初会诱导S期特异性pADPr信号传导,这是由未连接的冈崎片段导致的,最终导致pADPr不受控制地积累以及PARP1/2依赖性细胞毒性。此外,我们证明参与冈崎片段连接和/或碱基切除修复的蛋白质可调节PARG抑制诱导的pADPr信号传导和细胞死亡。此外,我们确定PARG的表达对于细胞对PARG抑制的敏感性至关重要。此外,我们发现PARG通过抑制pADPr对细胞存活至关重要。总的来说,我们的数据不仅确定了PARG在正常增殖细胞中的重要作用,还为PARG抑制剂在癌症治疗中的进一步开发提供了潜在的生物标志物。