Department of Pharmacology, Toxicology and Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas 66160, USA.
Department of Molecular and Integrative Physiology, The University of Kansas Medical Center, Kansas City, Kansas 66160, USA.
Toxicol Sci. 2021 Nov 24;184(2):276-285. doi: 10.1093/toxsci/kfab115.
Overdose of acetaminophen (APAP) is the major cause of acute liver failure (ALF) in the Western world with very limited treatment options. Previous studies from our groups and others have shown that timely activation of liver regeneration is a critical determinant of transplant-free survival of APAP-induced ALF patients. Here, we report that hepatocyte-specific deletion of Yes-associated protein (Yap), the downstream mediator of the Hippo Kinase signaling pathway results in faster recovery from APAP-induced acute liver injury. Initial studies performed with male C57BL/6J mice showed a rapid activation of Yap and its target genes within first 24 h after APAP administration. Treatment of hepatocyte-specific Yap knockout (Yap-KO) mice with 300 mg/kg APAP resulted in equal initial liver injury but a significantly accelerated recovery in Yap-KO mice. The recovery was accompanied by significantly rapid hepatocyte proliferation supported by faster activation of Wnt/β-catenin pathway. Furthermore, Yap-KO mice had significantly earlier and higher pro-regenerative inflammatory response following APAP overdose. Global gene expression analysis indicated that Yap-KO mice had a robust activation of transcription factors involved in response to endoplasmic reticulum stress (XBP1) and maintaining hepatocyte differentiation (HNF4α). In conclusion, these data indicate that inhibition of Yap in hepatocytes results in rapid recovery from APAP overdose due to an earlier activation of liver regeneration.
对乙酰氨基酚(APAP)过量是西方世界急性肝衰竭(ALF)的主要原因,治疗选择非常有限。我们小组和其他小组的先前研究表明,及时激活肝再生是 APAP 诱导的 ALF 患者无移植生存的关键决定因素。在这里,我们报告称,肝细胞特异性缺失 Yes 相关蛋白(Yap),即 Hippo 激酶信号通路的下游介质,可导致 APAP 诱导的急性肝损伤更快恢复。最初在雄性 C57BL/6J 小鼠中进行的研究表明,在给予 APAP 后的前 24 小时内,Yap 及其靶基因迅速被激活。用 300mg/kg APAP 治疗肝细胞特异性 Yap 敲除(Yap-KO)小鼠导致初始肝损伤相等,但 Yap-KO 小鼠的恢复明显加快。恢复伴随着更快的 Wnt/β-catenin 通路激活,支持更快的肝细胞增殖。此外,Yap-KO 小鼠在 APAP 过量后具有更早和更高的促再生炎症反应。全基因表达分析表明, Yap-KO 小鼠中涉及内质网应激(XBP1)和维持肝细胞分化(HNF4α)的转录因子被强烈激活。总之,这些数据表明,肝细胞中 Yap 的抑制导致 APAP 过量后迅速恢复,这是由于肝再生的更早激活。