HepG2 and Huh7 cell lines are frequently used as models to study viral hepatitis and hepatocellular carcinoma. However, they exhibit significantly different capacities in their ability to support hepatitis B virus (HBV) replication. To investigate the basis for this, transcription factor-binding motifs at the HBV core promoter (HBVCP) were tested in luciferase reporter constructs to identify the possible role of host factors. Among the transcription factors screened: PARP1, SP1, HNF4α, HNF3, hB1F and HNF1, deletion of the PARP1 binding motif abrogated transcriptional activity at the HBVCP in HepG2 but not Huh7 cells. Sequencing of the PARP1 gene revealed that HepG2 cells carried an Ala762 allele which has low ADP-ribosylation activity, which was shown to have increased PARP1 binding affinity to its cognate motif thus resulting in higher transcriptional activity. PARP1 inhibitors that are being developed as broad cancer therapeutics also target PARP1 ADP-ribosylation enzymatic function. Four PARP1 inhibitors: PJ-34, ABT888, AZD2281 and AG014699 were tested for their effect on HBV replication. All four small molecules effectively enhanced HBV replication in vitro, confirming the role of PARP1 in HBV replication and that alteration of ADP-ribosylation by mutation or drugs can affect HBV replication. Our data demonstrate that natural polymorphisms in the host affecting proteins such as PARP1 can have a significant effect on HBV replication. Hence, patients who are infected with HBV and are on clinical trials involving PARP1 inhibitors may be at risk from unintended side-effects such as exacerbation of HBV replication.

译文

HepG2和Huh7细胞系经常用作研究病毒性肝炎和肝细胞癌的模型。然而,它们在支持乙型肝炎病毒 (HBV) 复制的能力方面表现出明显不同的能力。为了研究这一点的基础,在荧光素酶报告构建体中测试了HBV核心启动子 (HBVCP) 的转录因子结合基序,以确定宿主因子的可能作用。在筛选的转录因子中: PARP1,SP1,HNF4α,HNF3,hB1F和HNF1,PARP1结合基序的缺失消除了HepG2中HBVCP的转录活性,而不是Huh7细胞。PARP1基因的测序表明,HepG2细胞携带Ala762等位基因,该等位基因具有较低的ADP-核糖基化活性,这被证明具有增加的PARP1与其同源基序的结合亲和力,从而导致更高的转录活性。作为广泛的癌症治疗药物正在开发的PARP1抑制剂也针对PARP1 ADP-核糖基化酶功能。测试了四种PARP1抑制剂: PJ-34,ABT888,AZD2281和AG014699对HBV复制的影响。所有四个小分子在体外有效地增强了HBV复制,证实了PARP1在HBV复制中的作用,并且通过突变或药物改变ADP-核糖基化可以影响HBV复制。我们的数据表明,宿主中影响蛋白 (如PARP1) 的自然多态性对HBV复制有显著影响。因此,感染HBV并正在进行涉及PARP1抑制剂的临床试验的患者可能会受到意外副作用 (例如HBV复制恶化) 的风险。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录