Department of Metabolic Regulation, Shinshu University Graduate School of Medicine, Matsumoto, Nagano, Japan.
Department of Metabolic Regulation, Shinshu University Graduate School of Medicine, Matsumoto, Nagano, Japan.
Pharmacol Ther. 2017 Nov;179:142-157. doi: 10.1016/j.pharmthera.2017.05.011. Epub 2017 May 23.
Ligand-activated nuclear receptors, including peroxisome proliferator-activated receptor alpha (PPARα), pregnane X receptor, and constitutive androstane receptor, were first identified as key regulators of the responses against chemical toxicants. However, numerous studies using mouse disease models and human samples have revealed critical roles for these receptors and others, such as PPARβ/δ, PPARγ, farnesoid X receptor (FXR), and liver X receptor (LXR), in maintaining nutrient/energy homeostasis in part through modulation of the gut-liver-adipose axis. Recently, disorders associated with disrupted nutrient/energy homeostasis, e.g., obesity, metabolic syndrome, and non-alcoholic fatty liver disease (NAFLD), are increasing worldwide. Notably, in NAFLD, a progressive subtype exists, designated as non-alcoholic steatohepatitis (NASH) that is characterized by typical histological features resembling alcoholic steatohepatitis (ASH), and NASH/ASH are recognized as major causes of hepatitis virus-unrelated liver cirrhosis and hepatocellular carcinoma. Since hepatic steatosis is basically caused by an imbalance between fat/energy influx and utilization, abnormal signaling of these nuclear receptors contribute to the pathogenesis of fatty liver disease. Standard therapeutic interventions have not been fully established for fatty liver disease, but some new agents that activate or inhibit nuclear receptor signaling have shown promise as possible therapeutic targets. In this review, we summarize recent findings on the roles of nuclear receptors in fatty liver disease and discuss future perspectives to develop promising pharmacological strategies targeting nuclear receptors for NAFLD/NASH.
配体激活的核受体,包括过氧化物酶体增殖物激活受体 α (PPARα)、妊娠相关 X 受体和组成型雄烷受体,最初被鉴定为应对化学毒物反应的关键调节剂。然而,大量使用小鼠疾病模型和人类样本的研究揭示了这些受体和其他受体(如 PPARβ/δ、PPARγ、法尼醇 X 受体 (FXR) 和肝 X 受体 (LXR))在维持营养/能量平衡中的关键作用,部分是通过调节肠道-肝脏-脂肪轴实现的。最近,与营养/能量平衡失调相关的疾病,如肥胖症、代谢综合征和非酒精性脂肪性肝病 (NAFLD),在全球范围内呈上升趋势。值得注意的是,在 NAFLD 中,存在一种进行性亚型,称为非酒精性脂肪性肝炎 (NASH),其特征是具有类似于酒精性脂肪性肝炎 (ASH)的典型组织学特征,并且 NASH/ASH 被认为是与肝炎病毒无关的肝硬化和肝细胞癌的主要原因。由于肝脂肪变性基本上是由脂肪/能量流入和利用之间的失衡引起的,这些核受体的异常信号转导导致脂肪性肝病的发病机制。尽管针对脂肪性肝病的标准治疗干预措施尚未完全建立,但一些激活或抑制核受体信号转导的新型药物已显示出作为潜在治疗靶点的希望。在这篇综述中,我们总结了核受体在脂肪性肝病中的作用的最新发现,并讨论了开发针对 NAFLD/NASH 的有前途的核受体靶向药理学策略的未来展望。