The potential for biased signalling in the P2Y receptor family of GPCRs
British Journal of Pharmacology, EarlyView.The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk +2 more
wiley +1 more source
BIASED AGONISM OF THREE DIFFERENT CANNABINOID RECEPTOR AGONISTS IN MOUSE BRAIN CORTEX
Frontiers in Pharmacology, 2016 Cannabinoid receptors are able to couple to different families of G-proteins when activated by an agonist drug. It has been suggested that different intracellular responses may be activated depending on the ligand.
Rebeca Diez-Alarcia +12 more
doaj +1 more source
Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment [PDF]
, 2013 Thermostabilized G protein-coupled receptors used as antigens for in vivo immunization have resulted in the generation of functional agonistic anti-β1-adrenergic (β1AR) receptor monoclonal antibodies (mAbs).
Ali Jazayeri +18 more
core +2 more sources
Novel approaches for drug development against chronic primary pain: A systematic review
British Journal of Pharmacology, EarlyView.Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus +5 more
wiley +1 more source
A Single Dose-Escalation Study to Evaluate the Safety and Pharmacokinetics of Orally Administered Des-Aspartate Angiotensin I in Healthy Subjects [PDF]
, 2016 Des-aspartate-angiotensin I (DAA-I) is an endogenous angiotensin peptide and a prototype angiotensin receptor agonist (ARA). It acts on the angiotensin AT(1) receptor and antagonises the deleterious actions of angiotensin II.
Balram Chowbay +4 more
core +1 more source
Editorial: Biased agonism in chemoattractant receptor signaling [PDF]
Journal of Leukocyte Biology, 2010 Abstract Selective induction of neutrophil responses by chemoattractants reflects biased agonistic activities of the ligands and is modulated at several levels in chemoattractant receptor signaling.
openaire +1 more source
Guest Editors' Introduction II: reflections on scholarship and activism in Canada and Ireland [PDF]
, 2015 No ...
Cantillon, Sara, Smeltzer, Sandra
core +3 more sources
Postprandial Glucagon Action in the Human Brain
Diabetes, Obesity and Metabolism, EarlyView.ABSTRACT Aims Elevated fasting glucagon is linked to hyperglycemia, but postprandial glucagon effects are less understood. Recent evidence suggests metabolic benefits of rising glucagon after oral glucose intake, potentially impacting brain‐mediated whole‐body metabolism.
Robert Wagner +11 more
wiley +1 more source
Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy. [PDF]
, 2018 Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands of these receptors display biased agonism and this may provide future therapeutic advantage.
Andreassen +70 more
core +2 more sources
Biased Agonism or “Biaism” for Dummies: A Commentary
ReceptorsThat signaling bias is a nth level of complexity in the understanding of G protein-coupled receptor (GPCR) activation is a first fact. That its exhaustive description, including the mode d’emploi of its quantitative measurement, remains a challenge is a second fact.
Jean A. Boutin, Jérôme Leprince
openaire +1 more source