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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

Aged G Protein-Coupled Receptor Kinase 3 (Grk3)-Deficient Mice Exhibit Enhanced Osteoclastogenesis and Develop Bone Lesions Analogous to Human Paget’s Disease of Bone

open access: greenCells, 2023
Paget’s Disease of Bone (PDB) is a metabolic bone disease that is characterized by dysregulated osteoclast function leading to focal abnormalities of bone remodeling. It can lead to pain, fracture, and bone deformity. G protein-coupled receptor kinase 3 (
Emily M. Rabjohns   +15 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

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

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