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G Protein-Coupled Receptor Kinases Take Central Stage [PDF]

open access: yesCells, 2022
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   +2 more sources

G protein coupled receptor in apoptosis and apoptotic cell clearance [PDF]

open access: yesFASEB BioAdvances
Apoptosis is a genetically programmed form of cell death that is substantially conserved across the evolutionary tree. Apoptotic cell elimination includes recognition, phagocytosis, and degradation. Failure to clear apoptotic cells can ultimately cause a
Xinyan Li   +8 more
doaj   +2 more sources

The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)

open access: yesBiomolecules, 2021
G protein-coupled receptors (GPCRs), which regulate a vast number of eukaryotic processes, are desensitized by various mechanisms but, most importantly, by the GPCR kinases (GRKs).
M. Claire Cato   +6 more
doaj   +1 more source

DEER Analysis of GPCR Conformational Heterogeneity

open access: yesBiomolecules, 2021
G protein-coupled receptors (GPCRs) represent a large class of transmembrane helical proteins which are involved in numerous physiological signaling pathways and therefore represent crucial pharmacological targets.
Matthias Elgeti, Wayne L. Hubbell
doaj   +1 more source

Allosteric modulation of G protein-coupled receptor signaling

open access: yesFrontiers in Endocrinology, 2023
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

Creation of photocyclic vertebrate rhodopsin by single amino acid substitution

open access: yeseLife, 2022
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

Interaction of the Xanthine Nucleotide Binding Goα Mutant with G Protein-coupled Receptors [PDF]

open access: yes, 1998
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

Functional optimization of light-activatable Opto-GPCRs: Illuminating the importance of the proximal C-terminus in G-protein specificity. [PDF]

open access: yes, 2023
Introduction: G-protein coupled receptors (GPCRs) are the largest family of human receptors that transmit signals from natural ligands and pharmaceutical drugs into essentially every physiological process.
Kleinlogel, Sonja, Leemann, Siri
core   +1 more source

Comparative Docking to Distinct G Protein–Coupled Receptor Conformations Exclusively Yields Ligands with Agonist Efficacy [PDF]

open access: yes, 2019
G protein-coupled receptors exist in a whole spectrum of conformations which are stabilised by the binding of ligands with different efficacy or intracellular effector proteins.
Baker, Jillian G.   +3 more
core   +2 more sources

C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor

open access: yeseLife, 2015
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

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