Department of Genetics, University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Division of Translational Medicine and Human Genetics, Department of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Clin Transl Sci. 2021 Jul;14(4):1369-1379. doi: 10.1111/cts.12988. Epub 2021 Jun 22.
Hepatocytes store triglycerides (TGs) in the form of lipid droplets (LDs), which are increased in hepatosteatosis. The regulation of hepatic LDs is poorly understood and new therapies to reduce hepatosteatosis are needed. We performed a siRNA kinase and phosphatase screen in HuH-7 cells using high-content automated imaging of LDs. Changes in accumulated lipids were quantified with developed pipeline that measures intensity, area, and number of LDs. Selected "hits," which reduced lipid accumulation, were further validated with other lipid and expression assays. Among several siRNAs that resulted in significantly reduced LDs, one was targeted to the nuclear adapter protein, transformation/transcription domain-associated protein (TRRAP). Knockdown of TRRAP reduced triglyceride accumulation in HuH-7 hepatocytes, in part by reducing C/EBPα-mediated de novo synthesis of TGs. These findings implicate TRRAP as a novel regulator of hepatic TG metabolism and nominate it as a potential drug target for hepatosteatosis.
肝细胞以脂滴 (LDs) 的形式储存甘油三酯 (TGs),肝脂肪变性时 LDs 会增加。肝 LDs 的调节机制尚不清楚,需要新的疗法来减少肝脂肪变性。我们使用高内涵自动化成像技术在 HuH-7 细胞中进行了 siRNA 激酶和磷酸酶筛选。通过开发的测量 LD 强度、面积和数量的管道来定量分析积累的脂质变化。选择减少脂质积累的“命中”结果,并用其他脂质和表达分析进行进一步验证。在导致 LD 明显减少的几种 siRNA 中,有一种针对核衔接蛋白转化/转录结构域相关蛋白 (TRRAP)。TRRAP 的敲低减少了 HuH-7 肝细胞中甘油三酯的积累,部分原因是降低了 C/EBPα 介导的 TG 的从头合成。这些发现表明 TRRAP 是肝 TG 代谢的一个新的调节因子,并将其作为肝脂肪变性的潜在药物靶点。