Structural basis for activation of trimeric Gi proteins by multiple growth factor receptors via GIV/Girdin. [PDF]
, 2014 A long-standing issue in the field of signal transduction is to understand the cross-talk between receptor tyrosine kinases (RTKs) and heterotrimeric G proteins, two major and distinct signaling hubs that control eukaryotic cell behavior.
Abagyan, Ruben +8 more
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GRKs as Modulators of Neurotransmitter Receptors
Cells, 2020 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
G protein-coupled receptor kinase 2 (GRK2) is localized to centrosomes and mediates epidermal growth factor-promoted centrosomal separation. [PDF]
, 2013 G protein-coupled receptor kinases (GRKs) play a central role in regulating receptor signaling, but recent studies suggest a broader role in modulating normal cellular functions.
Benovic, Jeffrey L +4 more
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Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
, 2003 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
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Sphingosine 1-phosphate receptors: do they have a therapeutic potential in cardiac fibrosis? [PDF]
, 2017 Sphingosine 1-phosphate (S1P) is a bioactive lipid that is characterized by a peculiar mechanism of action. In fact, S1P, which is produced inside the cell, can act as an intracellular mediator, whereas after its export outside the cell, it can act as ...
Frati, Alessia +4 more
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The Basal Thermal Sensitivity of the TRPV1 Ion Channel Is Determined by PKCβII [PDF]
, 2014 Copyright © 2014 the authors 0270-6474/14/348246-13$15.00/0.Peer reviewedPublisher ...
Hasan, Raquibul, Li, Lin, Zhang, Xuming
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G protein—coupled receptor kinase (GRK)
Folia Pharmacologica Japonica, 2010 Gタンパク質共役受容体キナーゼ（G Protein-coupled Receptor Kinase: GRK）の分子機能，分子構造，生理的役割を解説する．GRKは，Gタンパク質共役受容体（G Protein-Coupled Receptor: GPCR）をリン酸化するセリン・トレオニンキナーゼである．基本的な作用機構は，(1)アゴニスト結合した受容体（GPCR）がGRKを活性化，(2)活性化されたGRKが受容体をリン酸化，(3)リン酸化された受容体にアレスチン（arrestin）が結合，(4)その結果受容体の脱感受性（desensitization）が起こる，というものである．脱感受性は，受容体とGタンパク質との相互作用が損なわれる脱共役（uncoupling），受容体の細胞内への移行 ...
openaire +3 more sources
Caveolae-Independent Activation of Protein Kinase A in Rat Neonatal Myocytes
Journal of Pharmacological Sciences, 2005 Cardiomyocytes express both β1- and β2-adrenergic receptors, and these receptors play a differential role in chronotropic and inotropic effects of the heart. Caveolae are known as an important regulator of G-protein-coupled receptor signaling.
Masashi Fukutomi +4 more
doaj +1 more source
Endothelial APC/PAR1 distinctly regulates cytokine-induced pro-inflammatory VCAM-1 expression
Frontiers in Molecular Biosciences, 2023 Introduction: Dysfunction of the endothelium impairs its’ protective role and promotes inflammation and progression of vascular diseases. Activated Protein C (APC) elicits endothelial cytoprotective responses including barrier stabilization, anti ...
Cierra A. Birch +6 more
doaj +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]
, 2001 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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