Allosterism in the adenosine A2A and cannabinoid CB2 heteromer
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose Allosterism is a regulatory mechanism for GPCRs that can be attained by ligand‐binding or protein–protein interactions with another GPCR. We have studied the influence of the dimer interface on the allosteric properties of the A2A receptor and CB2 receptor heteromer.
Claudia Llinas del Torrent +7 more
wiley +1 more source
Effect of intrauterine morphine sulfate exposure on cerebellar histomorphological changes in neonatal mice [PDF]
, 2011 Neurotoxic effects of morphine sulfate in adult cerebellar cortex and neonatal cerebral cortex have been studied in animal models. This study was done to determine the neurotoxic effects of prenatal morphine exposure on the histo morphological changes of
Ghafari, S. +2 more
core
Progress on the development of Class A GPCR‐biased ligands
British Journal of Pharmacology, EarlyView.Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales +20 more
wiley +1 more source
Machine Learning Harnesses Molecular Dynamics to Discover New $μ$ Opioid Chemotypes [PDF]
arXiv, 2018 Computational chemists typically assay drug candidates by virtually screening compounds against crystal structures of a protein despite the fact that some targets, like the $\mu$ Opioid Receptor and other members of the GPCR family, traverse many non-crystallographic states.
arxiv
British Journal of Pharmacology, EarlyView.G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing signals from the extracellular environment to the inside of the cell. They mediate the effects of various stimuli, including hormones, neurotransmitters, ions, photons, food tastants and odorants, and are renowned drug targets.
Małgorzata M. Kogut‐Günthel +11 more
wiley +1 more source
In Vitro Analyses of Spinach-Derived Opioid Peptides, Rubiscolins: Receptor Selectivity and Intracellular Activities through G Protein- and β-Arrestin-Mediated Pathways. [PDF]
Molecules, 2021 Karasawa Y +12 more
europepmc +1 more source
European Journal of Clinical Investigation, EarlyView.This consensus highlights critical research gaps in obesity epidemiology, phenotypic heterogeneity and clinical management, calling for advanced methodologies, collaborative strategies and innovative policies to mitigate the global obesity epidemic and its socio‐economic impacts.
Federico Carbone +28 more
wiley +1 more source
Neuro-physiological characterization of opioid peptide actions on neurohumoral transmission in the mammalian central nervous system [PDF]
, 1986 Mercuri, Nicola +4 more
core +1 more source
A note on the evaluation of a beta-casein variant in bovine breeds by allele-specific PCR and relevance to β-casomorphin [PDF]
, 2008 peer-reviewedThis work was supported by Enterprise Ireland and by a Teagasc Walsh fellowship to A.F. Keating.Two genetic variants of the bovine β-casein gene (A1 and B) encode a histidine residue at codon 67, resulting in potential liberation of a ...
Cairns, M.T. +3 more
core
Survey on 9 years of anti‐doping controls in horse races in Italy
Equine Veterinary Journal, EarlyView.Abstract Background Doping in racehorses is a threat to horse welfare and the integrity of the sport. Despite its relevance, the literature on the prevalence of anti‐doping violations worldwide is limited. Objectives To analyse anti‐doping violations in racehorses in Italy. Study Design Retrospective observational study.
Mariana Roccaro +5 more
wiley +1 more source