[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 …

Virtual screening strategies in drug discovery: a critical review

A Lavecchia, C Di Giovanni - Current medicinal chemistry, 2013 - ingentaconnect.com
Virtual screening (VS) is a powerful technique for identifying hit molecules as starting points
for medicinal chemistry. The number of methods and softwares which use the ligand and …

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Z Zhao, X Dai, C Li, X Wang, J Tian, Y Feng… - European journal of …, 2020 - Elsevier
The pyrazolone structural motif is a critical element of drugs aimed at different biological end-
points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates …

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 …

ROR nuclear receptors: structures, related diseases, and drug discovery

Y Zhang, X Luo, D Wu, Y Xu - Acta Pharmacologica Sinica, 2015 - nature.com
Nuclear receptors (NRs) are ligand-regulated transcription factors that regulate metabolism,
development and immunity. The NR superfamily is one of the major classes of drug targets …

Organocatalytic Asymmetric Synthesis of Six‐Membered Carbocycle‐Based Spiro Compounds

X Xie, W Huang, C Peng, B Han - Advanced Synthesis & …, 2018 - Wiley Online Library
Well‐developed asymmetric organocatalysis has been widely incorporated in various
cascade/tandem sequences, providing a simple access to structurally complex target …

Opportunities and challenges for fatty acid mimetics in drug discovery

E Proschak, P Heitel, L Kalinowsky… - Journal of medicinal …, 2017 - ACS Publications
Fatty acids beyond their role as an endogenous energy source and storage are increasingly
considered as signaling molecules regulating various physiological effects in metabolism …

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 …

Beyond bile acids: targeting Farnesoid X Receptor (FXR) with natural and synthetic ligands

A Carotti, M Marinozzi, C Custodi… - Current topics in …, 2014 - ingentaconnect.com
The modulation of FXR receptor remains an attractive area in drug discovery to develop
novel therapeutic opportunities for liver and metabolic disorders. Despite the large variety of …

Structural Basis for Small Molecule NDB (N-Benzyl-N-(3-(tert-butyl)-4-hydroxyphenyl)-2, 6-dichloro-4-(dimethylamino) Benzamide) as a Selective Antagonist of …

X Xu, X Xu, P Liu, Z Zhu, J Chen, H Fu, L Chen… - Journal of Biological …, 2015 - ASBMB
Farnesoid X receptor α (FXRα) as a bile acid sensor plays potent roles in multiple metabolic
processes, and its antagonist has recently revealed special interests in the treatment of …