Results 51 to 60 of about 121,181 (303)
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
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
Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]
Bioorganic & Medicinal Chemistry Letters, 2016 Les modulateurs allostériques négatifs (MNA) CB1 existants appartiennent à une gamme limitée de classes structurelles. Malgré le potentiel théorique des NAM CB1, les études in vivo publiées n'ont généralement pas été en mesure de démontrer les effets thérapeutiques attendus médiés par CB1.
Iain R. Greig +4 more
openaire +3 more sources
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
An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor [PDF]
, 2020 Most drugs acting on G-protein-coupled receptors target the orthosteric binding pocket where the native hormone or neurotransmitter binds. There is much interest in finding allosteric ligands for these targets because they modulate physiologic signaling ...
Hirata, Kunio +31 more
core +1 more source
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
Journal of Clinical Psychiatry, 2020 OBJECTIVE To assess putative antidepressant and procognitive effects of decoglurant, a selective metabotropic glutamate receptor type 2/3 (mGlu2/3) negative allosteric modulator, as adjunctive treatment to selective serotonin reuptake inhibitors and/or ...
D. Umbricht +7 more
semanticscholar +1 more source
Discovery of Novel Gq-Biased LPA1 Negative Allosteric Modulators [PDF]
SLAS Discovery, 2017 Lysophosphatidic acid (LPA) activates the G-protein-coupled receptor LPA1, which regulates various cellular processes, including cell proliferation and migration. Although LPA1 transduces cellular responses via Gq, Gi, and G12/13, associations between these signaling molecules and cellular phenotypes remain poorly characterized due to the lack of ...
Yuji, Shimizu, Masaharu, Nakayama
openaire +2 more sources
Journal of Medicinal Chemistry, 2020 GPR84 is a medium chain free fatty acid-binding G protein-coupled receptor associated with inflammatory and fibrotic diseases. As the only reported antagonist of GPR84 (PBI-4050) displays relatively low potency and selectivity, a clear need exists for an
F. Labéguère +30 more
semanticscholar +1 more source