Pharmazentrum Frankfurt/ZAFES, Institute of Clinical Pharmacology, Johann Wolfgang Goethe University, House 74, Theodor Stern-Kai 7, 60590, Frankfurt am Main, Germany.
School of Biotechnology and Biomolecular Sciences, University of New South Wales, Sydney, NSW, 2052, Australia.
Cell Mol Life Sci. 2021 Nov;78(21-22):7025-7041. doi: 10.1007/s00018-021-03958-9. Epub 2021 Oct 9.
Hepatocellular carcinoma (HCC) is one of the most difficult cancer types to treat. Liver cancer is often diagnosed at late stages and therapeutic treatment is frequently accompanied by development of multidrug resistance. This leads to poor outcomes for cancer patients. Understanding the fundamental molecular mechanisms leading to liver cancer development is crucial for developing new therapeutic approaches, which are more efficient in treating cancer. Mice with a liver specific UDP-glucose ceramide glucosyltransferase (UGCG) knockout (KO) show delayed diethylnitrosamine (DEN)-induced liver tumor growth. Accordingly, the rationale for our study was to determine whether UGCG overexpression is sufficient to drive cancer phenotypes in liver cells. We investigated the effect of UGCG overexpression (OE) on normal murine liver (NMuLi) cells. Increased UGCG expression results in decreased mitochondrial respiration and glycolysis, which is reversible by treatment with EtDO-P4, an UGCG inhibitor. Furthermore, tumor markers such as FGF21 and EPCAM are lowered following UGCG OE, which could be related to glucosylceramide (GlcCer) and lactosylceramide (LacCer) accumulation in glycosphingolipid-enriched microdomains (GEMs) and subsequently altered signaling protein phosphorylation. These cellular processes lead to decreased proliferation in NMuLi/UGCG OE cells. Our data show that increased UGCG expression itself does not induce pro-cancerous processes in normal liver cells, which indicates that increased GlcCer expression leads to different outcomes in different cancer types.
肝细胞癌(HCC)是最难治疗的癌症类型之一。肝癌通常在晚期诊断,治疗时常伴有多药耐药性的发展。这导致癌症患者的预后较差。了解导致肝癌发展的基本分子机制对于开发新的治疗方法至关重要,这些方法在治疗癌症方面更有效。具有肝脏特异性 UDP-葡萄糖神经酰胺葡萄糖基转移酶(UGCG)敲除(KO)的小鼠显示出延迟的二乙基亚硝胺(DEN)诱导的肝肿瘤生长。因此,我们研究的基本原理是确定 UGCG 的过表达是否足以在肝细胞中驱动癌症表型。我们研究了 UGCG 过表达(OE)对正常鼠肝(NMuLi)细胞的影响。UGCG 表达增加导致线粒体呼吸和糖酵解减少,用 UGCG 抑制剂 EtDO-P4 处理可逆转这种减少。此外,FGF21 和 EPCAM 等肿瘤标志物在 UGCG OE 后降低,这可能与鞘糖脂(GlcCer)和乳糖基鞘氨醇(LacCer)在糖脂富集微区(GEMs)中的积累有关,随后改变信号蛋白磷酸化。这些细胞过程导致 NMuLi/UGCG OE 细胞增殖减少。我们的数据表明,UGCG 表达的增加本身不会在正常肝细胞中诱导致癌过程,这表明 GlcCer 表达的增加会导致不同癌症类型的不同结果。