Machine learning-and structure-based discovery of a novel chemotype as FXR agonists for potential treatment of nonalcoholic fatty liver disease

T Qin, X Gao, L Lei, J Feng, W Zhang, Y Hu… - European Journal of …, 2023 - Elsevier
Farnesoid X receptor (FXR) is a promising target for drug discovery against nonalcoholic
fatty liver disease (NAFLD). However, no FXR agonist has been approved for NAFLD so far …

Structural optimization and biological evaluation of 1-adamantylcarbonyl-4-phenylpiperazine derivatives as FXR agonists for NAFLD

T Qin, X Gao, L Lei, W Zhang, J Feng, X Wang… - European Journal of …, 2023 - Elsevier
Farnesoid X receptor (FXR) is an attractive target for drug discovery against non-alcoholic
fatty liver disease (NAFLD). We previously reported an orally active, new-chemotype FXR …

Design, synthesis and structure-activity relationship studies of novel partial FXR agonists for the treatment of fatty liver

Q Qiu, W Wang, X Zhao, Y Chen, S Zhao, J Zhu… - Bioorganic …, 2020 - Elsevier
Nonalcoholic fatty liver disease (NAFLD) is now the most common chronic liver disease,
while there is still no medicine available. Farnesoid X receptor (FXR) is considered as a …

Pharmacophore modeling and virtual screening studies for discovery of novel farnesoid X receptor (FXR) agonists

S Zhao, W Peng, X Li, L Wang, W Yin, YD Wang… - RSC …, 2021 - pubs.rsc.org
Farnesoid X receptor (FXR) agonists would be considered as an important therapeutic
strategy for several chronic liver and metabolic diseases. Here we have employed an …

Discovery of 4-aminophenylacetamide derivatives as intestine-specific farnesoid X receptor antagonists for the potential treatment of nonalcoholic steatohepatitis

C Chen, B Zhang, J Tu, Y Peng, Y Zhou, X Yang… - European Journal of …, 2024 - Elsevier
Farnesoid X receptor (FXR) plays a key role in bile acid homeostasis, inflammation, fibrosis,
lipid and glucose metabolism and is emerging as a promising therapeutic target for …

Discovery and optimization of non-bile acid FXR agonists as preclinical candidates for the treatment of nonalcoholic steatohepatitis

J Li, M Liu, Y Li, D Sun, Z Shu, Q Tan… - Journal of Medicinal …, 2020 - ACS Publications
Farnesoid X receptor (FXR) plays a key role in bile acid homeostasis, inflammation, fibrosis,
and metabolism of lipid and glucose and becomes a promising therapeutic target for …

Discovery of HPG1860, a structurally novel nonbile acid FXR agonist currently in clinical development for the treatment of nonalcoholic steatohepatitis

C Mo, X Xu, P Zhang, Y Peng, X Zhao… - Journal of Medicinal …, 2023 - ACS Publications
The farnesoid X receptor (FXR) is a ligand-activated nuclear receptor. Activation of FXR
significantly impacts the expressions of the pivotal genes involved in bile acid metabolism …

[HTML][HTML] Farnesoid X receptor as a promising therapeutic target for nonalcoholic fatty liver disease (NAFLD) and the current development of its agonists

T Shen, A Shi, Y Wei, X Luo, L Xi - Discovery Medicine, 2021 - discoverymedicine.com
Nonalcoholic fatty liver disease (NAFLD) comprises a group of clinical syndromes
characterized by excessive fat deposition in liver cells. Owing to its increasing incidence …

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 …

3D-QSAR and Molecular Dynamics Study of Isoxazole Derivatives to Identify the Structural Requirements for Farnesoid X Receptor (FXR) Agonists

D Yan, Y Yang, H Shen, Z Liu, K Yao, Q Liu - Molecules, 2024 - mdpi.com
The farnesoid X receptor (FXR) has been recognized as a potential drug target for the
treatment of non-alcoholic fatty liver disease (NAFLD). FXR agonists benefit NAFLD by …