Nutrient-sensing nuclear receptors PPARα and FXR control
2017年4月3日 · The nuclear receptors PPARα (encoded by NR1C1) and farnesoid X receptor (FXR, encoded by NR1H4) are activated in the liver in the fasted and fed state, respectively. PPARα activation induces fatty acid oxidation, while FXR controls bile acid homeostasis, but both nuclear receptors also regulate nume …
通过脂肪细胞中PPARγ激活的FXR表达促进脂肪生成。,Biochemical …
2020年4月24日 · 在scd基因启动子中发现了fxr反应元件（fxre），并且fxr与scd基因启动子的fxre结合，并且cdca在脂肪细胞中增强了其结合效率。这些结果表明，fxr通过以脂肪细胞中pparγ依赖性的方式增强scd的表达来辅助脂肪形成，从而使本研究首次确定fxr通过激活pparγ来促进脂肪 ...
过氧化物酶体增殖物激活受体 (PPAR)在肝脏疾病中的作用及潜在 …
摘要: 过氧化物酶体增殖物激活受体(ppar)是细胞核雌激素受体家族成员，参与多种体内生理病理过程，在细胞代谢、炎症及癌症等方面发挥重要作用，目前已知ppar受体分3种亚型，分别为α、β/δ和γ。研究发现ppar在肝脏中高度表达，广泛参与肝脏能量代谢、氧化 ...
The roles and interaction of FXR and PPARs in the pathogenesis …
2020年9月1日 · FXR and PPARs are mainly involved in nutrient acquisition from the gut and distribution through the liver to peripheral tissues including adipose and muscle. PPARs contain three isotypes encoded by the PPAR-α, PPAR-β/δ (or PPAR-β) and PPAR-γ genes.
A new perspective on NAFLD: Focusing on the crosstalk between ...
2022年10月1日 · Based on PPARα, dual PPAR and pan-PPAR agonists with moderate potency, balance and fewer side effects have shown greater therapeutic benefit in targeting NAFLD, and intestinal, liver-specific and structurally optimized FXR drugs are the way forward.
Cell Metabolism | FXR激活可通过胆汁酸依赖方式降低脂质吸收从 …
由于fxr是 胆汁酸代谢 的主要调节剂，因此fxr激活可能通过降低胆汁酸水平和/或改变胆汁酸组成来影响肠道脂质吸收。 通过UPLC-MS/MS 对肝脏、肠道和胆囊中胆汁酸进行定量检测，发现GSK2324激活FXR后可显著降低野生型小鼠总胆汁酸，而 Fxr-/- 小鼠未发生这种变化。
Discovery of FXR/PPARγ dual partial agonist - PubMed
2023年5月1日 · Farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor (PPAR)γ are nuclear receptor 1 superfamily of transcription factors. FXR and PPARγ agonists have been individually investigated in clinical trial of anti-diabetic agents in the patients with nonalcoholic fatty liver disease (N …
A triple farnesoid X receptor and peroxisome proliferator-activated ...
2020年11月13日 · Aiming to fuse complementary validated anti-NASH strategies in a single molecule, we have designed and systematically optimized a scaffold for triple activation of farnesoid X receptor (FXR),...
Nutrient-sensing nuclear receptors PPAR α and FXR control …
2017年3月13日 · The nuclear receptors PPARα (encoded by NR1C1) and farnesoid X receptor (FXR, encoded by NR1H4) are activated in the liver in the fasted and fed state, respectively. PPARα activation induces fatty acid oxidation, while FXR controls bile acid homeostasis, but both nuclear receptors also regulate numerous other metabolic pathways relevant to ...
The roles and interaction of FXR and PPARs in the pathogenesis …
Background and study aims: To identify the roles and interaction of farnesoid X receptor (FXR) and peroxisome proliferator activated receptors (PPARs) in Non-alcoholic fatty liver disease (NAFLD) pathogenesis.