Results 51 to 60 of about 24,311 (208)
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
Emerging Roles of β-Arrestins [PDF]
Cell Cycle, 2006 Arrestins were originally characterized as structural adaptor proteins which modulate the desensitization and trafficking of seven-membrane-spanning receptors. From these seminal observations a multitude of novel functions for this gene family have arisen. Here we review the recently identified roles for beta-arrestin including its nuclear function and
F Gregory, Buchanan, Raymond N, DuBois
openaire +2 more sources
Acta Ophthalmologica, EarlyView.Abstract Purpose To assess in Royal College of Surgeons (RCS) rats if the combination of two previously documented neuroprotective strategies: minocycline administration and bone marrow–derived mononuclear cells (BM‐MNCs) intravitreal transplantation, offers enhanced neuroprotection compared with each treatment alone.
Alba Videla‐Ristol +6 more
wiley +1 more source
Structural studies of phosphorylation-dependent interactions between the V2R receptor and arrestin-2
Nature Communications, 2021 The interaction between a GPCR, such as the vasopressin receptor-2 (V2R), and arrestin depends on the receptors’ phosphorylation pattern. Here authors use FRET and NMR to analyze the phosphorylation patterns of the V2R-arrestin complex and show that ...
Qing-Tao He +15 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
A small molecule enhances arrestin-3 binding to the β2-adrenergic receptor
Communications ChemistryExcessive signaling by various GPCRs underlies a variety of human disorders. Suppression of GPCRs by “enhanced” arrestin mutants was proposed as therapy.
Han Kurt +13 more
doaj +1 more source
Cell ReportsSummary: G protein-coupled receptors (GPCRs) exhibit signaling bias or preferential activation of heterotrimeric G proteins versus GPCR kinase (GRK)-mediated β-arrestin signaling.
Monica L. Gonzalez Ramirez +7 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
PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes
British Journal of Pharmacology, EarlyView.Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier +9 more
wiley +1 more source
Interaction of Arrestin with Enolase1 in Photoreceptors [PDF]
Investigative Opthalmology & Visual Science, 2011 Arrestin is in disequilibrium in photoreceptors, translocating between inner and outer segments in response to light. The purpose of this project was to identify the cellular component with which arrestin associates in the dark-adapted retina.Retinas were cross-linked with 2.5 mM dithiobis(succinimidylpropionate) (DSP), and arrestin-containing ...
W Clay, Smith +7 more
openaire +2 more sources