Bile acid and receptors: Biology and drug discovery for nonalcoholic fatty liver disease

T Jiao, Y Ma, X Guo, Y Ye, C Xie - Acta Pharmacologica Sinica, 2022 - nature.com
Nonalcoholic fatty liver disease (NAFLD), a series of liver metabolic disorders manifested by
lipid accumulation within hepatocytes, has become the primary cause of chronic liver …

International union of basic and clinical pharmacology CXIII: Nuclear receptor superfamily—Update 2023

TP Burris, IMS de Vera, I Cote, CA Flaveny… - Pharmacological …, 2023 - ASPET
The NR superfamily comprises 48 transcription factors in humans that control a plethora of
gene network programs involved in a wide range of physiologic processes. This review will …

SUMOylation inhibitors synergize with FXR agonists in combating liver fibrosis

J Zhou, S Cui, Q He, Y Guo, X Pan, P Zhang… - Nature …, 2020 - nature.com
Farnesoid X receptor (FXR) is a promising target for nonalcoholic steatohepatitis (NASH)
and fibrosis. Although various FXR agonists have shown anti-fibrotic effects in diverse …

FXR modulators for enterohepatic and metabolic diseases

H Wang, Q He, G Wang, X Xu, H Hao - Expert Opinion on …, 2018 - Taylor & Francis
ABSTRACT Introduction: Farnesoid X receptor (FXR), a nuclear receptor mainly expressed
in enterohepatic tissues, is a master for bile acid, lipid and glucose homeostasis …

[HTML][HTML] Combined obeticholic acid and apoptosis inhibitor treatment alleviates liver fibrosis

J Zhou, N Huang, Y Guo, S Cui, C Ge, Q He… - … Pharmaceutica Sinica B, 2019 - Elsevier
Obeticholic acid (OCA), the first FXR-targeting drug, has been claimed effective in the
therapy of liver fibrosis. However, recent clinical trials indicated that OCA might not be …

Bile acid metabolism and signaling in health and disease: molecular mechanisms and therapeutic targets

JS Fleishman, S Kumar - Signal Transduction and Targeted Therapy, 2024 - nature.com
Bile acids, once considered mere dietary surfactants, now emerge as critical modulators of
macronutrient (lipid, carbohydrate, protein) metabolism and the systemic pro …

FXR: structures, biology, and drug development for NASH and fibrosis diseases

S Tian, S Chen, C Pan, Y Li - Acta Pharmacologica Sinica, 2022 - nature.com
The nuclear receptor farnesoid-X-receptor (FXR) plays an essential role in bile acid,
glucose, and lipid homeostasis. In the last two decades, several diseases, such as obesity …

Discovery of the first-in-class intestinal restricted FXR and FABP1 dual modulator ZLY28 for the treatment of nonalcoholic fatty liver disease

Q Ren, Y Chen, Z Zhou, Z Cai, S Jiao… - Journal of Medicinal …, 2023 - ACS Publications
The prevalence of nonalcoholic steatohepatitis (NASH) is increasing rapidly worldwide, and
NASH has become a serious problem for human health. Recently, the selective activation of …

[HTML][HTML] Targeting bile acid signaling for the treatment of liver diseases: From bench to bed

S Duan, X Li, G Fan, R Liu - Biomedicine & Pharmacotherapy, 2022 - Elsevier
Liver diseases and related complications have become one of the leading causes of
morbidity and mortality worldwide, yet effective medicine or approved treatment approach is …

Discovery of LH10, a novel fexaramine-based FXR agonist for the treatment of liver disease

W Huang, Z Cao, W Wang, Z Yang, S Jiao, Y Chen… - Bioorganic …, 2024 - Elsevier
Farnesoid X receptor (FXR) was considered as a promising drug target in the treatment of
cholestasis, drug-induced liver injury, and non-alcoholic steatohepatitis (NASH). However …