Thrombus Formation under Shear "Glycoprotein (GP)VI and integrin αIIbβ3 are key signaling receptors The multiple downstream signaling pathways are still poorly understood. Here, we focused on disclosing the integrin-dependent roles of focal adhesion kinase (protein tyrosine PTK2), the shear-dependent collagen receptor GPR56 (ADGRG1 gene), and calcium and integrin-binding protein This work thereby supports the role of PTK2 in integrin αIIbβ3 activation and signaling."

of monomeric β2-AR, unlike the inverse agonists, implying that the cholesterol is a specific factor regulating

G protein-coupled receptors (GPCRs) have been shown to play integral roles in Alzheimer's disease pathogenesis 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

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron Several neurotransmitters and neuromodulators, acting through G-protein-coupled receptors (GPCRs), fine-tune by the physiological neuromodulator lysophosphatidic acid (LPA) through a mechanism entailing Gαi/o-protein IME by TASK1 inhibition, stimulated ROCK2, and depressed background resting currents via Gαq/ROCK2 signaling These outcomes suggest that LPA and several neurotransmitters impact MN IME via Gαi/o/Gαq-protein-coupled

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior, and neurophysiology "The awareness of the potential importance of functional selectivity/biased signaling A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent vs. β-arrestin related signaling. important pharmacological, molecular, and cellular studies relevant to D1-mediated β-arrestin-related signaling

Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in primary Sjögren's remains unknown, and there is no ideal drug for the specific treatment of pSS. β-arrestin2 is a key protein that mediates desensitization and internalization of G protein-coupled receptors (GPCRs) and it participates In vivo, we found that inhibition of GRP78-ATF6-CHOP apoptosis signaling improved ESS symptoms, and the , decreased cell viability, and induced apoptosis, which were negatively regulated by the ERS inhibitor

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."

September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and hetero-dimer formation "The process of GPCR dimerization can have profound effects on GPCR activation, signaling The cytoskeletal protein filamin A (FLNA) directly interacts with both somatostatin receptor type 2 ( SST2) and 5 (SST5) and regulates their expression and signaling in pituitary tumoral cells. Moreover, we showed that FLNA regulates SST2 and SST5 intracellular trafficking induced by octreotide

production of bioactive C3a, a product of C3 cleavage, which interacts with membrane-bound receptor C3aR to regulate previous research has identified mechanistically distinct and cell type–specific roles for C3aR in regulating specific responses during bacterial infections and emphasize the contribution of the C3a–C3aR axis in regulating

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

October 2022 "The very large G protein-coupled receptor (VLGR1, ADGRV1) is the largest member of the Affinity proteomics revealed that in the interactome of VLGR1, molecules are enriched that are associated We confirmed the interaction of VLGR1 with key proteins of MAMs by pull-down assays in vitro complemented functional interaction of VLGR1 with components in MAMs and point to an essential role of VLGR1 in the regulation

September 2022 "RNA editing is a process by which post-transcriptional changes of mRNA nucleotides alter protein The 5HT2C serotonin receptor, which undergoes 32 distinct RNA-editing events leading to 24 protein isoforms also provide a comprehensive analysis of agonist activation and constitutive activity across all 24 protein intracellular loop 2 that is subject to RNA editing, which differentially affects GPCR constitutive and agonist signaling

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered We further highlight residues in transmembrane 7 (TM7) that mediate stronger signaling in mouse versus

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by initially identified as a PAR2 antagonist, is a bona fide agonist of PAR2 that induces unique cellular signaling phosphorylation of MAPKs, but in a delayed and sustained manner compared to the rapid and transient signals results revealed that GB83 is a bona fide agonist of PAR2 that uniquely modulates PAR2-mediated cellular signaling

October 2022 "Perturbation of the endocannabinoid system can have profound effects on immune function and synaptic plasticity. Microglia are one of few cell types with a self-contained endocannabinoid system and are positioned at the interface between the immune system and the central nervous system. Past work has produced conflicting results with respect to the effects of pro-inflammatory conditions on the microglial endocannabinoid system. Thus, we systematically investigated the relationship between the concentration of two distinct pro-inflammatory stimuli, lipopolysaccharide and interferon gamma, on the abundance of components of the endocannabinoid system within microglia. Here we show that lipopolysaccharide and interferon gamma influence messenger RNA abundances of the microglial endocannabinoid system in a concentration-dependent manner. Furthermore, we demonstrate that the efficacy of different synthetic cannabinoid treatments with respect to inhibition of microglia nitric oxide release is dependent on the concentration and type of pro-inflammatory stimuli presented to the microglia. This indicates that different pro-inflammatory stimuli influence the capacity of microglia to synthesize, degrade, and respond to cannabinoids which has implications for the development of cannabinoid-based treatments for neuroinflammation." Read more at the source #DrGPCR #GPCR #IndustryNews

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

Promising nuclear receptors as key regulators of transcriptional programmes will be introduced as well Fibroblasts from SSc patients exhibit a specific signalling and reactivate developmental pathways and Pharmacological interventions, although for other indications, are already in clinical use to address pathologic signalling

The C5aR1 is a classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that tailors immune cell activity potentially through β-arrestins rather than G-proteins.

Sara Marsango and Graeme Milligan for their research on the Regulation of the pro-inflammatory G protein-coupled of the pro-inflammatory G protein-coupled receptor GPR84 Function and regulation of GPR84 in human neutrophils Large-scale deorphanization of Nematostella vectensis neuropeptide G protein-coupled receptors supports interactions that contribute to G protein coupling Reviews, GPCRs, and more Molecular adaptations in of the glucagon receptor family Technologies for the discovery of G protein-coupled receptor-targeting

Serotonin receptor 5-HT2A and tropomyosin receptor kinase B (TrkB) strongly contribute to neuroplasticity regulation An expression analysis revealed strong developmental regulation of 5-HT2A and TrkB expressions in the Our data reveal the functional role of 5-HT2A–TrkB receptor heterodimerization and suggest that the regulated

We have previously reported that the MC4R forms homodimers, affecting receptor Gs signaling properties setmelanotide, a novel synthetic MC4R agonist, suggest a predominant role of the Gq/11 pathway regarding weight regulation In this study, we analyzed effects of inhibiting homodimerization on Gq/11 signaling using previously NanoBRETTM studies to determine protein–protein interaction were conducted, confirming decreased homodimerization of setmelanotide signaling at wild-type MC4R (MC4R-WT).

September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent evaluate the role of dual transactivation of EGF and TGF-β receptors in phosphorylation of Smad2L and protein In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Proteins were investigated<br />by western blotting using protein-specific antibodies against phospho-Smad2 This study is the first attempt to scrutinize the significant role of ROCK in the protein expression

Here, we sought to investigate the role of Regulator of G Protein Signaling 7 (RGS7) in hyperlipidemia-dependent

August 2022 " Background and purpose: Vascular tone is regulated by the relative contractile state of Several integrins directly modulate VSMC contraction by regulating calcium influx through L-type voltage-gated We determined whether SVEP1 and integrin α9β1 can regulate VSMC contraction."

differentiation of MECs by assessing changes in cellular viability, lipid accumulation, and gene and protein expression of major milk protein and lipid synthesizing markers. using the HC11 cells as a model. We hypothesized that THC and CBD will negatively impact the synthesis of milk proteins and lipids, as Relative to control, 10μM THC and 10μM CBD reduced mRNA levels of milk proteins (CSN2 and WAP) , lipid and glucose transport markers (GLUT 1 , HK2 , FASN , FABP4 , PLIN2 and LPL) , as well as whey acidic protein

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular regions that bind to multiple ligands to regulate key biological functions including neurodevelopment

mediating function of neuronal G protein-coupled receptors (GPCRs) in controlling the response to polystyrene and some neuronal GPCRs (such as DOP-2, NPR-8, DAF-37, and DCAR-1) functioned upstream of GPA-10 to regulate Therefore, neuronal Gα proteins of GOA-1, GSA-1, and GPA-10 functioned to transduce signals of multiple GPCRs to different downstream signaling pathways during the control of PS-NPs toxicity in nematodes. Our results provide clues for understanding the important function of GPCRs-Gα signaling cascade in the

Moreover, the mechanisms underlying regulation of TRPM3 are largely unexplored.