G protein-coupled receptor kinase (GRK)-mediated receptor phosphorylation and β-arrestin binding uncouple G protein-coupled receptors (GPCRs) from their respective G proteins and initiates the process of receptor internalization.
J. Pitcher +5 more
semanticscholar +1 more source
GRKs as Modulators of Neurotransmitter Receptors
Many receptors for neurotransmitters, such as dopamine, norepinephrine, acetylcholine, and neuropeptides, belong to the superfamily of G protein-coupled receptors (GPCRs). A general model posits that GPCRs undergo two-step homologous desensitization: the
Eugenia V. Gurevich +1 more
doaj +1 more source
Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio +4 more
core +1 more source
A polymorphic variant of the human α2B-adrenergic receptor (α2BAR), which consists of a deletion of three glutamic acids (residues 301–303) in the third intracellular loop was found to be common in Caucasians (31%) and to a lesser extent in African ...
K. Small +3 more
semanticscholar +1 more source
Synaptic plasticity via receptor tyrosine kinase/G-protein-coupled receptor crosstalk
Summary: Cellular signaling involves a large repertoire of membrane receptors operating in overlapping spatiotemporal regimes and targeting many common intracellular effectors.
Cristina Lao-Peregrin +11 more
doaj +1 more source
The Role of G Protein-coupled Receptor Kinases in Cancer [PDF]
G protein-coupled receptors (GPCRs) are the largest family of plasma membrane receptors. Emerging evidence demonstrates that signaling through GPCRs affects numerous aspects of cancer biology such as vascular remolding, invasion, and migration. Therefore, development of GPCR-targeted drugs could provide a new therapeutic strategy to treating a variety ...
Yu, Shan +3 more
openaire +2 more sources
Tailoring therapy for heart failure: the pharmacogenomics of adrenergic receptor signaling. [PDF]
Heart failure is one of the leading causes of mortality in Western countries, and β-blockers are a cornerstone of its treatment. However, the response to these drugs is variable among individuals, which might be explained, at least in part, by genetic ...
Barrese, V +3 more
core +2 more sources
The Role of G-Protein-Coupled Receptor Kinase 5 in Pathogenesis of Sporadic Parkinson's Disease
Sporadic Parkinson's disease (sPD) is a common neurodegenerative disorder, characterized by selective degeneration of dopaminergic neurons in the substantia nigra.
S. Arawaka +34 more
semanticscholar +1 more source
Phosphatidylinositol 4‐kinase as a target of pathogens—friend or foe?
This graphical summary illustrates the roles of phosphatidylinositol 4‐kinases (PI4Ks). PI4Ks regulate key cellular processes and can be hijacked by pathogens, such as viruses, bacteria and parasites, to support their intracellular replication. Their dual role as essential host enzymes and pathogen cofactors makes them promising drug targets.
Ana C. Mendes +3 more
wiley +1 more source
Threonine 180 Is Required for G-protein-coupled Receptor Kinase 3- and β-Arrestin 2-mediated Desensitization of the µ-Opioid Receptor in Xenopus Oocytes [PDF]
To determine the sites in the µ-opioid receptor (MOR) critical for agonist-dependent desensitization, we constructed and coexpressed MORs lacking potential phosphorylation sites along with G-protein activated inwardly rectifying potassium channels ...
Celvert, Jeremy P. +4 more
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