Results 91 to 100 of about 13,057 (254)
Arrestin‐centred interactions at the membrane and their conformational determinants
British Journal of Pharmacology, Volume 182, Issue 14, Page 3135-3150, July 2025.Abstract More than 30 years after their discovery, arrestins are recognised multiprotein scaffolds that play essential roles in G protein‐coupled receptor (GPCR) regulation and signalling. Originally named for their capacity to hinder GPCR coupling to G proteins and facilitate receptor desensitisation, arrestins have emerged as key hubs for a myriad of
Owen Underwood +3 more
wiley +1 more source
Signaling Bias and Antagonism of Pilocarpine for M3 Muscarinic Acetylcholine Receptor
The FASEB Journal, 2018 Pilocarpine is a prototypical drug used to treat glaucoma and dry mouth since the 19th century and classified as either a full or partial muscarinic agonist. Here, we report several unexpected results pertaining to its interaction with its main therapeutic target ‐ muscarinic M3 receptor (M3R).
Kelly Wang +2 more
openaire +1 more source
Non-Neuronal Functions of the M2 Muscarinic Acetylcholine Receptor [PDF]
, 2013 Acetylcholine is an important neurotransmitter whose effects are mediated by two classes of receptors. The nicotinic acetylcholine receptors are ion channels, whereas the muscarinic receptors belong to the large family of G protein coupled seven ...
Acevedo +58 more
core +3 more sources
G protein‐coupled receptor‐mediated autophagy in health and disease
British Journal of Pharmacology, Volume 182, Issue 14, Page 3151-3162, July 2025.G protein‐coupled receptors (GPCRs) constitute the largest and most diverse superfamily of mammalian transmembrane proteins. These receptors are involved in a wide range of physiological functions and are targets for more than a third of available drugs in the market. Autophagy is a cellular process involved in degrading damaged proteins and organelles
Devrim Öz‐Arslan +2 more
wiley +1 more source
Role of M3 Muscarinic Acethylcholine Receptor Antibodies as a New Marker in Primary Sjögren Syndrome [PDF]
, 2017 Aims: This paper investigates the presence of M3 muscarinic acetylcholine receptor autoantibody present in the serum of patients with primary Sjögren syndrome (pSS).
Borda, Enri Santiago +4 more
core +1 more source
ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
British Journal of Pharmacology, Volume 182, Issue 14, Page 3178-3210, July 2025.G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison +15 more
wiley +1 more source
A novel M3 muscarinic acetylcholine receptor is expressed in chick atrium and ventricle.
Journal of Biological Chemistry, 1994 Prior studies have suggested that heart expresses only the M2 isoform of the muscarinic receptor (Peralta, E.G., Ashkenazi, A., Winslow, J.W., Smith, D.H., Ramachandran, J., and Capon, D.J. (1987) EMBO J. 6, 3923-3929). Tietje and Nathanson (Tietje, K.M., and Nathanson, N. M. (1991) J. Biol. Chem.
Albert P. Gadbut, Jonas B. Galper
openaire +3 more sources
Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]
, 2007 Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung +3 more
core +1 more source
BMC Gastroenterology, 2010 Background Autoantibodies to the human muscarinic acetylcholine receptor of the M3 type (hmAchR M3) have been suggested to play an etiopathogenic role in Sjögren's syndrome.
Berg Peter A +6 more
doaj +1 more source
Progress on the development of Class A GPCR‐biased ligands
British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.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