GPCR function has revealed new paradigms with increasingly complex models of receptor activation and signaling Spatial-temporal signaling of GPCRs and physiological functions; 2. The structural basis for GPCR activation of down-stream signaling and regulatory proteins; and 4.

discuss the historic context of pepducin development for each receptor, as well as the structural, signaling

Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling pathway for cholesterol sensing and couples cholesterol concentrations to mTORC1-dependent anabolic signaling

with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer which interact directly and indirectly with a wide number of cellular partners and mediate downstream signaling adaptor proteins that control the recruitment, activation, and scaffolding of numerous cytoplasmic signaling complexes and assist in G-protein receptor signaling, thus bringing them into close proximity. This review delivers a concise overview of the role of β-arrestins with a primary emphasis on the signaling

encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer which interact directly and indirectly with a wide number of cellular partners and mediate downstream signaling adaptor proteins that control the recruitment, activation, and scaffolding of numerous cytoplasmic signaling complexes and assist in G-protein receptor signaling, thus bringing them into close proximity. This review delivers a concise overview of the role of β-arrestins with a primary emphasis on the signaling

Furthermore, in sPD models, the shortening of PC is accompanied by increased Sonic Hedgehog (SHH) signal Inhibiting overactive SHH signaling may be a potential neuroprotective therapy for sPD."

March 2022 ERNEST has established an Emergency Fund for Ukrainian researchers. "General Eligibility Researchers affiliated to any legal entity in Ukraine (for example, schools and universities, research centers, governmental institutions, or private companies) Deadlines Start of the project: now End of the project: 31 October 2022 SHORT-TERM SCIENTIFIC MISSIONS (STSM) We offer short-term scientific mission grants to Ukrainian researchers who have been recently displaced by the war, or those who can travel to institutions participating in ERNEST COST Action. The purpose of the STSM is to carry out a collaborative research project on topics relevant to the network. Our scientific perspective is broad, and we are happy to consider any research proposals from those in need." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer Information flow from a source to a receiver becomes informative when the recipient can process the signal Information exchange and interpretation is essential in biology and understanding how cells integrate signals communication occurs mostly through neurotransmitters and hormones, and receptors are responsible for signal led to the hypothesis that their dimeric state can provide the framework for temporal coincidence in signaling

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid Here we investigated a potential mechanism for regulation of PLC signaling downstream of MOR in HEK293 cells and found that MOR alone could not stimulate PLC, but rather required a coincident signal from These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation

Although numerous signals are known to regulate synapses, it remains unclear which signaling mechanisms referred to as "SynTAMs" for synaptic targeting molecules, that enable localized perturbations of cAMP signaling In vivo, suppression of postsynaptic cAMP signaling in CA1 neurons prevented formation of both Schaffer-collateral Retrograde trans-synaptic rabies virus tracing revealed that postsynaptic cAMP signaling is required adhesion-GPCRs drive synapse formation and produce cAMP, we suggest that spatially restricted postsynaptic cAMP signals

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor In all cases, the receptor interaction changes downstream signalling and the responses to receptor agonists This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs,

Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein or β-arrestin signaling Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation reduced fertility, and memory impairment, which are potentially associated with impaired G protein signaling We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling maintaining the spacing between ROS discs, suggesting a plausible mechanism by which intrinsic optical signals

August 2022 "Genetically encoded fluorescent biosensors allow intracellular signaling dynamics to be FRET), and we have recently developed a simple approach for in vivo detection of FRET-based biosensor signals By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Recording from specific neuronal populations, we can quantify intracellular signaling while simultaneously

September 2022 GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic In this study, the expression and signaling of β2-ADR in B cells during collagen-induced arthritis (CIA downstream molecules (G protein-coupled receptor kinase 2 (GRK-2), β-Arrestin 2, p38 MAPK, extracellular signal-regulated The change of β2-ADR expression and signaling during sustained inflammation might be an integral part

September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent Thrombus Formation under Shear "Glycoprotein (GP)VI and integrin αIIbβ3 are key signaling receptors The multiple downstream signaling pathways are still poorly understood. Peptides did not influence GPVI-induced aggregation and Ca2+ signaling in the absence of shear. This work thereby supports the role of PTK2 in integrin αIIbβ3 activation and signaling."

protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization, internalization, and signaling not proximal, phosphorylation of the chemokine receptor CXCR4 specifies βarrestin1 (βarr1)-dependent signaling not proximal, C-tail phosphorylation sites are required for recruitment of the adaptor protein STAM1 (signal-transducing adaptor molecule) to βarr1 and focal adhesion kinase phosphorylation but not extracellular signal-regulated this study provides evidence that distal C-tail phosphorylation sites specify GRK-βarrestin-mediated signaling

GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate -81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative variants of 139, 141, and 173 amino acids, our current understanding on how endogenous PTHrP transduces signals and (iii) receptor internalization and recycling that the native PTHrP1-141 displays biased agonist signaling Furthermore, we show that the molecular basis for biased signaling differences between PTHrP1-36 and Taken together, our results contribute to a better understanding of the biased signaling process of a

correlate with three cholesterol molecules that play essential roles in conformation stabilization and signaling Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor) signaling

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the fine-tuning of Gi/o signaling "Aims: Cardiac contractility, essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled receptor (GPCR) signaling Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron IME by TASK1 inhibition, stimulated ROCK2, and depressed background resting currents via Gαq/ROCK2 signaling

GPCRs share a common mechanism of action via the β-arrestin scaffolding signaling complexes, which not only serve to desensitize GPCRs by internalization, but also mediate multiple downstream signaling events As signaling via the GPCRs, β2-adrenergic receptor (β2AR), and metabotropic glutamate receptor 2 (mGluR2

achieved for 6 by treatment with 1 µM CAN1404 for 24 h, and a corresponding increase in FSH-induced signaling