[HTML][HTML] Farnesoid X receptor (FXR): Structures and ligands

L Jiang, H Zhang, D Xiao, H Wei, Y Chen - Computational and structural …, 2021 - Elsevier
Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly
expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved …

Nuclear receptors and nonalcoholic fatty liver disease

MC Cave, HB Clair, JE Hardesty, KC Falkner… - … et Biophysica Acta (BBA …, 2016 - Elsevier
Nuclear receptors are transcription factors which sense changing environmental or
hormonal signals and effect transcriptional changes to regulate core life functions including …

[HTML][HTML] Progress and challenges of selective Farnesoid X Receptor modulation

V Massafra, R Pellicciari, A Gioiello… - Pharmacology & …, 2018 - Elsevier
Bile acids are amphipathic molecules that were previously known to serve as fat solubilizers
in the intestine in postprandial conditions. In the last two decades, bile acids have been …

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 …

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 …

18β-Glycyrrhetinic acid protects against alpha-naphthylisothiocyanate-induced cholestasis through activation of the Sirt1/FXR signaling pathway

S Wu, S Cui, L Wang, Y Zhang, X Yan, H Lu… - Acta pharmacologica …, 2018 - nature.com
Cholestasis is a common feature of liver injury, which manifests as bile acid excretion and/or
enterohepatic circulation disorders. However, very few effective therapies exist for …

Recent progress on bile acid receptor modulators for treatment of metabolic diseases

Y Xu - Journal of medicinal chemistry, 2016 - ACS Publications
Bile acids are steroid-derived molecules synthesized in the liver, secreted from hepatocytes
into the bile canaliculi, and subsequently stored in the gall bladder. During the feeding, bile …

[HTML][HTML] wSDTNBI: a novel network-based inference method for virtual screening

Z Wu, H Ma, Z Liu, L Zheng, Z Yu, S Cao, W Fang… - Chemical …, 2022 - pubs.rsc.org
In recent years, the rapid development of network-based methods for the prediction of drug–
target interactions (DTIs) provides an opportunity for the emergence of a new type of virtual …

Determination of molecule category of ligands targeting the ligand-binding pocket of nuclear receptors with structural elucidation and machine learning

Q Wang, Z Wang, S Tian, L Wang, R Tang… - Journal of Chemical …, 2022 - ACS Publications
The mechanism of transcriptional activation/repression of the nuclear receptors (NRs)
involves two main conformations of the NR protein, namely, the active (agonistic) and …

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 …