The Role of G Protein-coupled Receptor Kinases in Cancer [PDF]
International Journal of Biological Sciences, 2018 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
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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
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Synaptic plasticity via receptor tyrosine kinase/G-protein-coupled receptor crosstalk
Cell ReportsSummary: 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
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On the hierarchical classification of G Protein-Coupled Receptors [PDF]
, 2007 Motivation: G protein-coupled receptors (GPCRs) play an important role in many physiological systems by transducing an extracellular signal into an intracellular response. Over 50% of all marketed drugs are targeted towards a GPCR.
Matthew N. Davies +11 more
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Transactivation of G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs): Recent insights using luminescence and fluorescence technologies [PDF]
, 2021 © 2020 The Authors Alterations in signalling due to bidirectional transactivation of G protein-coupled receptor (GPCRs) and receptor tyrosine kinases (RTKs) are well established. Transactivation significantly diversifies signalling networks within a cell
Kilpatrick, Laura E., Hill, Stephen J.
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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 ...
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G protein-coupled receptor kinase 2-mediated phosphorylation of ezrin is required for G protein-coupled receptor-dependent reorganization of the actin cytoskeleton [PDF]
, 2005 G protein-coupled receptor kinase 2 (GRK2) phosphorylates and desensitizes activated G protein-coupled receptors (GPCRs). Here, we identify ezrin as a novel non-GPCR substrate of GRK2. GRK2 phosphorylates glutathione S-transferase (GST)-ezrin, but not an
Pitcher, JA, Cant, SH
core
Reciprocal control of viral infection and phosphoinositide dynamics
FEBS Letters, EarlyView.Phosphoinositides, although scarce, regulate key cellular processes, including membrane dynamics and signaling. Viruses exploit these lipids to support their entry, replication, assembly, and egress. The central role of phosphoinositides in infection highlights phosphoinositide metabolism as a promising antiviral target.
Marie Déborah Bancilhon, Bruno Mesmin
wiley +1 more source
Receptor for activated C kinase-1 facilitates protein kinase C-dependent phosphorylation and functional modulation of GABA(A) receptors with the activation of G-protein-coupled receptors [PDF]
, 2002 GABA(A) receptors are the principal sites of fast synaptic inhibition in the brain. These receptors are hetero-pentamers that can be assembled from a number of subunit classes: alpha(1-6), beta(1-3), gamma(1-3), delta(1), epsilon, theta, and pi, but the ...
Trevor G Smart +7 more
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Phosphatidylinositol 4‐kinase as a target of pathogens—friend or foe?
FEBS Letters, EarlyView.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