Results 41 to 50 of about 871,508 (182)

Beta-Arrestins and Receptor Signaling in the Vascular Endothelium

open access: yesBiomolecules, 2020
The vascular endothelium is the innermost layer of blood vessels and is a key regulator of vascular tone. Endothelial function is controlled by receptor signaling through G protein-coupled receptors, receptor tyrosine kinases and receptor serine ...
Claudia Lee   +5 more
doaj   +1 more source

Targeting β2‐Adrenergic Receptor Stability With Lycorine Reveals a Host‐Directed Pathway for Antiviral Defense Against Poxviruses

open access: yesAdvanced Science, EarlyView.
Chronic stress drives autophagy‐mediated β2‐AR degradation, impairing antiviral immunity and promoting poxvirus lethality. Lycorine directly stabilizes β2‐AR to restore host defense, suppress excessive inflammation and improve survival. ABSTRACT Psychological stress is a pervasive yet poorly understood modulator of infectious disease outcomes. Here, we
Xin Zhang   +12 more
wiley   +1 more source

EphB1 Receptor Blockade Augments Morphine Antinociception via Inhibiting GRK2‐Mediated µ‐Opioid Receptor Internalization

open access: yesAdvanced Science, EarlyView.
Administration of opioids activates ephrinB2‐EphB1 receptor signaling. Activated EphB1 receptors induce GRK2‐mediated phosphorylation of MOR at Ser375, which initiates the internalization of MOR and reduces opioid antinociception at the behavioral level. ABSTRACT Opioids are the primary treatment for severe pain in clinical practice.
Bo Peng   +7 more
wiley   +1 more source

β-arrestins are required for nebivolol-mediated phosphorylation of ERK.

open access: yes, 2013
siRNA directed towards β-arrestin 1 and 2 were transfected into MEFs; 72 hours later the cells were stimulated with 10 µM of nebivolol for 7 minutes. A representative blot for β-arrestins and total ERK is depicted in panel A above the histogram of the ...
Jenny Nguyen (448355)   +8 more
core   +1 more source

Multiple Scaffolding Functions of β-Arrestins in the Degradation of G Protein-coupled Receptor Kinase 2 [PDF]

open access: yes, 2011
G protein-coupled receptor kinase 2 (GRK2) plays a fundamental role in the regulation of G protein-coupled receptors (GPCRs), and changes in GRK2 expression levels can have an important impact on cell functions.
Federico Mayor   +9 more
core   +1 more source

Cannabinoid CB1 and CB2 Receptor-Mediated Arrestin Translocation: Species, Subtype, and Agonist-Dependence

open access: yesFrontiers in Pharmacology, 2019
Arrestin translocation and signaling have come to the fore of the G protein-coupled receptor molecular pharmacology field. Some receptor–arrestin interactions are relatively well understood and considered responsible for specific therapeutic or adverse ...
Mikkel Søes Ibsen   +9 more
doaj   +1 more source

Targeting Cannabinoid 1 Receptor in Macrophages Alleviates Psoriatic Skin Inflammation Through the AUF1–NLRP3 Axis

open access: yesAdvanced Science, EarlyView.
Macrophage CB1R emerges as a key driver of psoriatic inflammation by suppressing AUF1‐mediated post‐transcriptional control of NLRP3. CB1R inhibition restores AUF1‐dependent NLRP3 mRNA decay, restrains inflammasome activation, and alleviates psoriasis‐like inflammation.
Hongseo Choi   +22 more
wiley   +1 more source

β-arrestin recruitment facilitates a direct association with G proteins

open access: yesNature Communications
G protein-coupled receptors (GPCRs) are targets for almost a third of all FDA-approved drugs. GPCRs are known to signal through both heterotrimeric G proteins and β-arrestins. Traditionally these pathways were viewed as largely separable, with G proteins
Claudia Y. Lee   +15 more
doaj   +1 more source

Function and dynamics of the intrinsically disordered carboxyl terminus of β2 adrenergic receptor

open access: yesNature Communications, 2023
Advances in structural biology have provided important mechanistic insights into signaling by the transmembrane core of G-protein coupled receptors (GPCRs); however, much less is known about intrinsically disordered regions such as the carboxyl terminus (
Jie Heng   +19 more
doaj   +1 more source

Histamine and the mechanisms of nausea and vomiting: Translating the uncertain pharmacology of cyclizine

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Abstract Cyclizine is a long‐established, short‐acting drug, registered for preventing motion sickness, post‐operative nausea and vomiting (PONV) and ‘vomiting of known cause’. The latter is not defined but may include pregnancy and patients receiving palliative care, historically accepted without large, controlled trials.
Gareth J. Sanger, Paul L. R. Andrews
wiley   +1 more source

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