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Potential Roles of G Protein-Coupled Receptor 30 (GPR30) in Migraine Pathophysiology [PDF]

open access: yesJournal of Pain Research
Yuning Yao,1 Yang Gong,1,* Kegang Cao2,* 1Department of Traditional Chinese Medicine, General Hospital of the PLA Northern Theater Command, Shenyang, Liaoning, People’s Republic of China; 2Department of Neurology, Dongzhimen Hospital of ...
Yao Y, Gong Y, Cao K
doaj   +2 more sources

Structural insights into G protein-coupled receptor signaling [PDF]

open access: yesStructural Dynamics
G protein-coupled receptors (GPCRs) are the largest single family of transmembrane proteins encoded in the human genome, and they are among the most successful classes of therapeutic drug targets of all time.
Andrew Kruse
doaj   +2 more sources

High capacity in G protein-coupled receptor signaling [PDF]

open access: yesNature Communications, 2018
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

Mas‐Related G Protein‐Coupled Receptor Member D Sustains Hypertension [PDF]

open access: yesMedComm
Hypertension and its associated complications, including vascular remodeling, pose a major burden on global public health. However, the role of Mas‐related G protein‐coupled receptor member D (MrgD) in hypertension remains incompletely understood.
Kun Zhao   +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

G Protein-Coupled Receptor Kinases Take Central Stage

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   +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

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

Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]

open access: yes, 2009
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

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