Population Shift Mechanism for Partial Agonism of AMPA Receptor.
Sign Up to like & getrecommendations! Published in 2019 at "Biophysical journal"
DOI: 10.1016/j.bpj.2018.11.3122
Abstract: α-amino-3-hydroxy-5-methyl-4-isoaxazolepropionic acid (AMPA) ionotropic glutamate receptors mediate fast excitatory neurotransmission in the central nervous system, and their dysfunction is associated with neurological diseases. Glutamate binding to ligand-binding domains (LBDs) of AMPA receptors induces channel opening… read more here.
Keywords: ampa; population shift; agonism ampa; ampa receptor ... See more keywords
Partial agonism improves the anti-hyperglycaemic efficacy of an oxyntomodulin-derived GLP-1R/GCGR co-agonist
Sign Up to like & getrecommendations! Published in 2021 at "Molecular Metabolism"
DOI: 10.1016/j.molmet.2021.101242
Abstract: Objective Glucagon-like peptide-1 and glucagon receptor (GLP-1R/GCGR) co-agonism can maximise weight loss and improve glycaemic control in type 2 diabetes and obesity. In this study, we investigated the cellular and metabolic effects of modulating the… read more here.
Keywords: glp gcgr; arrestin recruitment; weight loss; efficacy ... See more keywords
Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01148
Abstract: Both dopamine D3 receptor (D3R) partial agonists and antagonists have been implicated as potential medications for substance use disorders. In contrast to antagonists, partial agonists may cause fewer side effects since they maintain some dopaminergic… read more here.
Keywords: structural basis; basis partial; dopamine receptor; partial agonism ... See more keywords
Molecular tuning of farnesoid X receptor partial agonism
Sign Up to like & getrecommendations! Published in 2019 at "Nature Communications"
DOI: 10.1038/s41467-019-10853-2
Abstract: The bile acid-sensing transcription factor farnesoid X receptor (FXR) regulates multiple metabolic processes. Modulation of FXR is desired to overcome several metabolic pathologies but pharmacological administration of full FXR agonists has been plagued by mechanism-based… read more here.
Keywords: partial agonism; fxr; fxr agonists; farnesoid receptor ... See more keywords