Results 31 to 40 of about 3,750,504 (279)
Development of allosteric modulators of GPCRs for treatment of CNS disorders
Neurobiology of Disease, 2014 The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols +1 more
doaj +1 more source
eLife, 2020 Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams +12 more
doaj +1 more source
Molecules, 2021 The CB1 cannabinoid receptor (CB1R) contains one of the longest N termini among class A G protein-coupled receptors. Mutagenesis studies suggest that the allosteric binding site of cannabidiol (CBD) involves residues from the N terminal domain.
Jakub Jakowiecki +5 more
doaj +1 more source
Natural Negative Allosteric Modulators of 5-HT3 Receptors [PDF]
Molecules, 2018 Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT3; serotonin) receptors in the pathogenesis and treatment of CINV.
Lina T. Al Kury +3 more
openaire +3 more sources
In silico Insights on the Allosteric Modulation of the µ-Opioid Receptor and G protein Complex in the Presence of Agonist Ligand BU72 and Potential Positive Allosteric Modulator BMS-986121 [PDF]
, 2020 The G protein-coupled receptor (GPCR) µ-opioid receptor (µOR) is one of several drug targets of commercially available therapeutics for pain. Various opioid drugs like morphines have been associated to numerous substance abuse-related deaths around the ...
Ricky, Nellas, Mac Kevin, Braza
core +1 more source
CHIMIA, 2021 Heteronuclear NMR in combination with isotope labelling is used to study folding of polypeptides induced by metals in the case of metallothioneins, binding of the peptidic allosteric modulator ρ-TIA to the human G-protein coupled α1b adrenergic receptor,
Oliver Zerbe +5 more
doaj +1 more source
Allostery of atypical modulators at oligomeric G protein-coupled receptors
Scientific Reports, 2021 Many G protein-coupled receptors (GPCRs) are therapeutic targets, with most drugs acting at the orthosteric site. Some GPCRs also possess allosteric sites, which have become a focus of drug discovery.
Rabindra V. Shivnaraine +7 more
doaj +1 more source
Identification of compounds acting as negative allosteric modulators of the LPA1 receptor [PDF]
European Journal of Pharmacology, 2018 The Lysophosphatidic Acid 1 Receptor (LPA1 receptor) has been linked to the initiation and progression of a variety of poorly treated fibrotic conditions. Several compounds that have been described as LPA1 receptor antagonists have progressed into clinical trials: 1-(4-{4-[3-methyl-4-({[(1R)-1-phenylethoxy]carbonyl}amino)-1,2-oxazol-5-yl]phenyl}phenyl ...
Ellery, Jonathan +11 more
openaire +3 more sources
Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer
eLife, 2017 GPCRs play critical roles in cell communication. Although GPCRs can form heteromers, their role in signaling remains elusive. Here we used rat metabotropic glutamate (mGlu) receptors as prototypical dimers to study the functional interaction between each
Junke Liu +13 more
doaj +1 more source