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High capacity in G protein-coupled receptor signaling [PDF]
G protein-coupled receptors (GPCRs) activate intracellular signalling pathways upon extracellular stimulation. Here authors record single cell responses of GPCR signalling which allows the direct estimation of its channel capacity for each cell along ...
Amiran Keshelava +6 more
doaj +4 more sources
G Protein-Coupled Receptor Kinases Take Central Stage
The relevance of the family of G protein-coupled receptor kinases (GRKs) is based on its key participation in the regulation and intracellular dynamics of the largest family of membrane receptors, namely G protein-coupled receptors (GPCRs) [...]
Federico Mayor, Cristina Murga
doaj +1 more source
G Protein–Coupled Receptor Heteromers [PDF]
G protein–coupled receptors (GPCRs) compose one of the largest families of membrane proteins involved in intracellular signaling. They are involved in numerous physiological and pathological processes and are prime candidates for drug development. Over the past decade, an increasing number of studies have reported heteromerization between GPCRs.
Gomes, Ivone +5 more
openaire +3 more sources
Allosteric modulation of G protein-coupled receptor signaling
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins, regulate a wide array of physiological processes in response to extracellular signals. Although these receptors have proven to be the most successful class of drug targets,
Siyuan Shen +6 more
doaj +1 more source
Interaction of the Xanthine Nucleotide Binding Goα Mutant with G Protein-coupled Receptors [PDF]
We constructed a double mutant version of the α subunit of Go that was regulated by xanthine nucleotides instead of guanine nucleotides (GoαX). We investigated the interaction between GoαX and G protein-coupled receptors in vitro.
Simon, Melvin I., Yu, Bo
core +1 more source
Creation of photocyclic vertebrate rhodopsin by single amino acid substitution
Opsins are universal photoreceptive proteins in animals and can be classified into three types based on their photoreaction properties. Upon light irradiation, vertebrate rhodopsin forms a metastable active state, which cannot revert back to the original
Kazumi Sakai +3 more
doaj +1 more source
Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros +31 more
core +3 more sources
Gi- and Gs-coupled GPCRs show different modes of G-protein binding. [PDF]
More than two decades ago, the activation mechanism for the membrane-bound photoreceptor and prototypical G protein-coupled receptor (GPCR) rhodopsin was uncovered.
Altenbach, Christian +7 more
core +1 more source
Rod photoreceptors generate measurable responses to single-photon activation of individual molecules of the G protein-coupled receptor (GPCR), rhodopsin.
Anthony W Azevedo +10 more
doaj +1 more source
G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core +1 more source

