Results 141 to 150 of about 406,175 (317)

Functional Activation of G-Proteins Coupled With Muscarinic Acetylcholine Receptors in Rat Brain Membranes

open access: yesJournal of Pharmacological Sciences, 2014
.: 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  

Deepening insights into cholinergic agents for intraocular pressure reduction: systems genetics, molecular modeling, and in vivo perspectives

open access: yesFrontiers in Molecular Biosciences
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

Gαq signalling from endosomes: A new conundrum

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3068-3089, July 2025.
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

open access: yesAngewandte Chemie, Volume 137, Issue 24, June 10, 2025.
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

open access: yesInternational Journal of COPD, 2015
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  

Arrestin‐centred interactions at the membrane and their conformational determinants

open access: yesBritish 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

G protein‐coupled receptor‐mediated autophagy in health and disease

open access: yesBritish 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

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