Results 41 to 50 of about 18,849 (159)
Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling
Nature Communications, 2017 Angiotensin II type 1 receptor (AT1R)-mediated acute catecholamine release is modulated by β-arrestin. Here the authors show that β-arrestin-1 recruits the Ca2+channel TRPC3 and the PLCγ to the AT1R-β-arrestin complex, triggering G protein-independent ...
Chun-Hua Liu +26 more
doaj +1 more source
Molecular mechanisms of fentanyl mediated β-arrestin biased signaling.
PLoS Computational Biology, 2020 The development of novel analgesics with improved safety profiles to combat the opioid epidemic represents a central question to G protein coupled receptor structural biology and pharmacology: What chemical features dictate G protein or β-arrestin ...
Parker W de Waal +7 more
doaj +1 more source
The Effects of Apelin and Elabela Ligands on Apelin Receptor Distinct Signaling Profiles
Frontiers in Pharmacology, 2021 Apelin and Elabela are endogenous peptide ligands for Apelin receptor (APJ), a widely expressed G protein-coupled receptor. They constitute a spatiotemporal dual ligand system to control APJ signal transduction and function.
Yunlu Jiang +11 more
doaj +1 more source
Sodium Ions Affect GPR17 Conformational States and Functionality
Proteins: Structure, Function, and Bioinformatics, EarlyView.ABSTRACT Sodium is an allosteric modulator of several class‐A GPCR regulating active versus inactive conformation state and may be a critical issue for the optimization of crystallization procedures. Herein, the role of Na+ in the regulation of GPR17 conformational states was studied through MD simulations of GPR17 wild‐type and mutated on two ...
Luca Palazzolo +6 more
wiley +1 more source
Lipids modulate the dynamics of GPCR:β-arrestin interaction
Nature Communicationsβ-arrestins are key molecular partners of G Protein-Coupled Receptors (GPCRs), triggering not only their desensitization but also intracellular signaling.
Antoniel A. S. Gomes +8 more
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Imaging Ligand-Dependent Activation of CXCR7
Neoplasia: An International Journal for Oncology Research, 2009 Chemokine CXCL12 is proposed to promote multiple steps in growth of primary tumors and progression to metastatic disease in more than 20 different cancers.
Kathryn E. Luker +4 more
doaj +1 more source
β-Arrestin1 and 2 differentially regulate PACAP-induced PAC1 receptor signaling and trafficking. [PDF]
PLoS ONE, 2018 A pituitary adenylate cyclase-activating polypeptide (PACAP)-specific receptor, PAC1R, is coupled with multiple signal transduction pathways including stimulation of adenylate cyclase, phospholipase C and extracellular-signal regulated kinase (ERK)1/2 ...
Yusuke Shintani +8 more
doaj +1 more source
Compartmentalisation in cAMP signalling: A phase separation perspective
British Journal of Pharmacology, EarlyView.Cells rely on precise spatiotemporal control of signalling pathways to ensure functional specificity. The compartmentalisation of cyclic AMP (cAMP) and protein kinase A (PKA) signalling enables distinct cellular responses within a crowded cytoplasmic space.
Milda Folkmanaite, Manuela Zaccolo
wiley +1 more source
ACKR3 Regulation of Neuronal Migration Requires ACKR3 Phosphorylation, but Not β-Arrestin
Cell Reports, 2019 Summary: Phosphorylation of heptahelical receptors is thought to regulate G protein signaling, receptor endocytosis, and non-canonical signaling via recruitment of β-arrestins.
Friederike Saaber +10 more
doaj +1 more source
The potential for biased signalling in the P2Y receptor family of GPCRs
British Journal of Pharmacology, EarlyView.The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk +2 more
wiley +1 more source