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Leaving no stone unturned: Allosteric targeting of SARS-CoV-2 Spike protein at putative druggable sites disrupts human angiotensin-converting enzyme interactions at the receptor binding domain.
The systematic entry of SARS-CoV-2 into host cells, as mediated by its Spike (S) protein, is
highly essential for pathogenicity in humans. Hence, targeting the viral entry mechanisms
remains a major strategy for COVID-19 ...
Flavonoids as GABAA receptor ligands: the whole story?
(Dove Medical Press, 2012-01)
Benzodiazepines are the most widely prescribed class of psychoactive drugs in current therapeutic use, despite the important unwanted side effects that they produce, such as sedation, myorelaxation, ataxia, amnesia, and ...
Phosphorylation of Ryanodine Receptors
(Sociedad de Biología de Chile, 2004)
Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein
(American Society for Biochemistry and Molecular Biology, 2004)
Accurate characterization of the molecular mechanisms of the action of ligands is an extremely important issue for their appropriate research, pharmacological, and therapeutic uses. In view of this fact, the aim of the ...
Ligand binding to CNS muscarinic receptor is transiently modified by convulsant 3-mercaptopropionic acid administration
(Springer/Plenum Publishers, 2000-06)
The administration of convulsant drugs has proven a powerful tool to study experimental epilepsy. We have already reported that the administration of convulsant 3-mercaptopropionic acid (mp) at 150 mg/kg enhances binding ...
Improved pan-specific prediction of MHC class I peptide binding using a novel receptor clustering data partitioning strategy
(Wiley Blackwell Publishing, Inc, 2016-12)
Pan-specific prediction of receptor–ligand interaction is conventionally done using machine-learning methods that integrates information about both receptor and ligand primary sequences. To achieve optimal performance using ...
More than meets the dimer: What is the quaternary structure of the glucocorticoid receptor?
(Taylor, 2017-01-08)
It is widely accepted that the glucocorticoid receptor (GR), a ligand-regulated transcription factor that triggers anti-inflammatory responses, binds specific response elements as a homodimer. Here, we will discuss the ...
Allosteric positive interaction of thymol with the GABA-A receptor in primary cultures of mouse cortical neurons
(Pergamon-Elsevier Science Ltd, 2006-01)
Thymol is a naturally occurring phenolic monoterpene known for its anti-microbial and anti-oxidant properties. It is used in dental practice and in anaesthetic halothane preparations. Recent studies have reported enhanced ...