Bile Acids and FXR: Novel Targets for Liver Diseases.

Bile Acids and FXR: Novel Targets for Liver Diseases.
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胆汁酸和FXR:肝脏疾病的新靶点。

DOI:
10.3389/fmed.2020.00544
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发表时间:
2020
影响因子:
3.9
通讯作者:
Guo GL
Guo GL
中科院分区:
医学3区
文献类型:
--
作者:
Stofan M;Guo GL

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胆汁酸(BAs)是由胆固醇在肝脏中合成的进化保守分子,已被证明是维持脂质平衡所必需的。BA通过调节核受体和膜受体来调节多种代谢功能。法尼醇X受体(FXR)是维持BA内环境稳定的最重要的核受体。FXR在抑制BA合成、促进BA肠肝循环方面具有组织特异性作用。在小鼠中,FXR的中断与人类常见的肝病有关,包括胆汁淤积症、非酒精性脂肪性肝病和肝细胞癌。针对FXR活性的战略性靶向已被迅速用于开发预防和/或治疗胆汁淤积症和非酒精性脂肪性肝炎的新疗法。本文就BA动态平衡和FXR调节剂的研究进展作一综述。
Bile acids (BAs) are evolutionally conserved molecules synthesized in the liver from cholesterol and have been shown to be essential for lipid homeostasis. BAs regulate a variety of metabolic functions via modulating nuclear and membrane receptors. Farnesoid X receptor (FXR) is the most important nuclear receptor for maintaining BA homeostasis. FXR plays a tissue-specific role in suppressing BA synthesis and promoting BA enterohepatic circulation. Disruption of FXR in mice have been implicated in liver diseases commonly occurring in humans, including cholestasis, non-alcoholic fatty liver diseases, and hepatocellular carcinoma. Strategically targeting FXR activity has been rapidly used to develop novel therapies for the prevention and/or treatment of cholestasis and non-alcoholic steatohepatitis. This review provides an updated literature review on BA homeostasis and FXR modulator development.
DOI: 10.1007/164_2019_227
发表时间: 2019-01-01
期刊: BILE ACIDS AND THEIR RECEPTORS
影响因子: --
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