.: The functional activation of Gi/o proteins coupled to muscarinic acetylcholine receptors (mAChRs) was investigated with the conventional guanosine-5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding assay in rat brain membranes.
Yuji Odagaki+2 more
doaj
Parasympathetic activation in the anterior eye segment regulates various physiological functions. This process, mediated by muscarinic acetylcholine receptors, also impacts intraocular pressure (IOP) through the trabecular meshwork. While FDA-approved M3
Minjae J. Kim+4 more
doaj +1 more source
Pairing the cholinergic agonist carbachol with patterned Schaffer collateral stimulation initiates protein synthesis in hippocampal CA1 pyramidal cell dendrites via a muscarinic, NMDA-dependent mechanism [PDF]
Sherry L. Feig, Peter Lipton
openalex +1 more source
Gαq signalling from endosomes: A new conundrum
Abstract G‐protein‐coupled receptors (GPCRs) constitute the largest family of membrane receptors, and are involved in the transmission of a variety of extracellular stimuli such as hormones, neurotransmitters, light and odorants into intracellular responses.
Carole Daly, Bianca Plouffe
wiley +1 more source
Synthesis and Characterization of Photoswitchable Covalent Ligands for the β2‐Adrenoceptor
A structure‐based design of a covalent photoswitchable ligand for the β2‐adrenergic receptor, a therapeutically relevant GPCR, is described. This tool facilitates the modification of the intrinsic activity of the protein by light. Computational analysis of its mechanism of action suggests that the photoswitch takes place within the binding pocket ...
Ulrike Wirth+9 more
wiley +2 more sources
The reasons for triple therapy in stable COPD patients in Japanese clinical practice
Masaki Miyazaki,1 Hidetoshi Nakamura,1,2 Saeko Takahashi,1 Shotaro Chubachi,1 Mamoru Sasaki,1 Mizuha Haraguchi,1 Hideki Terai,1 Makoto Ishii,1 Koichi Fukunaga,1 Sadatomo Tasaka,1 Kenzo Soejima,1 Koichiro Asano,3 Tomoko Betsuyaku1 On behalf of the Keio ...
Miyazaki M+12 more
doaj
Agonist‐induced Transfer of the α Subunits of the Guanine‐nucleotide‐binding Regulatory Proteins Gq and G11, and of Muscarinic m1 Acetylcholine Receptors from Plasma Membranes to a Light‐vesicular Membrane Fraction [PDF]
Petr Svoboda, Graeme Milligan
openalex +1 more source
Arrestin‐centred interactions at the membrane and their conformational determinants
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
G protein‐coupled receptor‐mediated autophagy in health and disease
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