ATHENA: A Phase 3, Open-Label Study Of The Safety And Effectiveness Of Oliceridine (TRV130), A G-Protein Selective Agonist At The µ-Opioid Receptor, In Patients With Moderate To Severe Acute Pain Requiring Parenteral Opioid Therapy. [PDF]
, 2019 Background:Pain management with conventional opioids can be challenging due to dose-limiting adverse events (AEs), some of which may be related to the simultaneous activation of β-arrestin (a signaling pathway associated with opioid-related AEs) and G ...
Beard, Timothy L +10 more
core
Reciprocal regulation of PKA and rac signaling [PDF]
, 2013 Activated G protein-coupled receptors (GPCRs) and receptor tyrosine kinases relay extracellular signals through spatial and temporal controlled kinase and GTPase entities.
A. Riml +47 more
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Targeting protein–protein interactions within the cyclic AMP signaling system as a therapeutic strategy for cardiovascular disease [PDF]
, 2013 The cAMP signaling system can trigger precise physiological cellular responses that depend on the fidelity of many protein–protein interactions, which act to bring together signaling intermediates at defined locations within cells.
Brunton +8 more
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Discovery of functionally selective C5aR2 ligands: novel modulators of C5a signalling. [PDF]
, 2016 The complement cascade is comprised of a highly sophisticated network of innate immune proteins that are activated in response to invading pathogens or tissue injury. The complement activation peptide, C5a, binds two seven transmembrane receptors, namely
Blaskovich, M.A. +11 more
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Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects [PDF]
, 2019 Opioid analgesics are powerful pain relievers; however, over time, pain control diminishes as analgesic tolerance develops. The molecular mechanisms initiating tolerance have remained unresolved to date.
Bailey, A +8 more
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The effect of arrestin conformation on the recruitment of c-Raf1, MEK1, and ERK1/2 activation.
PLoS ONE, 2011 Arrestins are multifunctional signaling adaptors originally discovered as proteins that "arrest" G protein activation by G protein-coupled receptors (GPCRs).
Sergio Coffa +6 more
doaj +1 more source
Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. [PDF]
, 2017 The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling.
Adams, Christopher M. +12 more
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Phosducin regulates the expression of transducin betagamma subunits in rod photoreceptors and does not contribute to phototransduction adaptation. [PDF]
, 2007 For over a decade, phosducin's interaction with the betagamma subunits of the G protein, transducin, has been thought to contribute to light adaptation by dynamically controlling the amount of transducin heterotrimer available for activation by ...
Arshavsky, Vadim Y +6 more
core
Unraveling the molecular architecture of a G protein-coupled receptor/β-arrestin/Erk module complex [PDF]
, 2015 International audienceβ-arrestins serve as signaling scaffolds downstream of G protein-coupled receptors, and thus play a crucial role in a plethora of cellular processes.
Azé, Jérôme +6 more
core +4 more sources
PAR1 Agonists Stimulate APC-Like Endothelial Cytoprotection and Confer Resistance to Thromboinflammatory Injury [PDF]
, 2018 Stimulation of protease-activated receptor 1 (PAR1) on endothelium by activated protein C (APC) is protective in several animal models of disease, and APC has been used clinically in severe sepsis and wound healing.
Aisiku, Omozuanvbo +10 more
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