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

GPCRs Functional partnerships between GPI-anchored proteins and adhesion GPCRs GPCR Activation and Signaling by a biased intracellular agonist The psychosis risk factor RBM12 encodes a novel repressor of GPCR/cAMP signal transduction The relaxin receptor RXFP1 signals through a mechanism of autoinhibition To probe from inactive conformation using molecular dynamic simulations Kinetic insights into agonist-dependent signalling , 2023) Training Seminar "The Renaissance in GPCRs as Drug Targets: Allosteric Function and Biased Signaling

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

GPCR Symposia Our upcoming symposium on March 15th is about GPCR activation and signaling. Let’s dive into the Classified GPCR News from February 5th to 11th, 2024 GPCR Activation and Signaling Insights into GPCR Function GPR161 structure uncovers the redundant role of sterol-regulated ciliary cAMP signaling in the Hedgehog pathway Unraveling the Interplay of Extracellular Domain Conformational Changes 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling

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

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

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,

Arrestins regulate a wide range of signaling events, most notably when bound to active G protein-coupled modulates Fgr activity with a hallmark bell-shaped concentration-dependence, consistent with a role as a 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

GPCR Symposia Our upcoming symposium on March 15th is about GPCR activation and signaling. signaling pathway The non-nutritive sweetener sucralose increases β-arrestin signaling at the constitutively GRK5 promoted renal fibrosis via HDAC5/Smad3 signaling pathway Non-canonical G protein signaling GPCR Molecular Insights into GPCR Function Structural insights into membrane adenylyl cyclases, initiators of cAMP signaling Molecular mechanism of GPCR spatial organization at the plasma membrane Industry News Launch

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

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

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 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 translatability of cell and animal models to have more precise functional targeting to harness the value of this signaling

Intracellular calcium ([Ca2+]i) signaling is a critical regulator of chondrogenesis, chondrocyte differentiation Calcium (Ca2+) signaling is known to direct processes that govern chondrocyte gene expression, protein Control of chondrocyte/chondroprogenitor Ca2+ signaling has been attempted through mechanical and/or Synthetic signaling platforms permitting precise and selective Ca2+ signal transduction can improve dissection of the roles that [Ca2+]i signaling plays in chondrocyte behavior.

October 2022 "Psychedelics, also known as classical hallucinogens, affect processes related to perception, cognition and sensory processing mostly via the serotonin 5-HT2A receptor (5-HT2AR). This class of psychoactive substances, which includes lysergic acid diethylamide (LSD), psilocybin, mescaline and the substituted amphetamine 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), is receiving renewed attention for their potential therapeutic properties as it relates to psychiatric conditions such as depression and substance use disorders. Current studies focused on the potentially clinical effects of psychedelics on human subjects tend to exclude sex as a biological variable. Much of the understanding of psychedelic pharmacology is derived from rodent models, but most of this preclinical research has only focused on male mice. Here we tested the effects of DOI on head-twitch behavior (HTR) - a mouse behavioral proxy of human psychedelic potential - in male and female mice. DOI elicited more HTR in female as compared to male C57BL/6J mice, a sex-specific exacerbated behavior that was not observed in 129S6/SvEv animals. Volinanserin (or M100907) - a 5-HT2AR antagonist - fully prevented DOI-induced HTR in male and female C57BL/6J mice. Accumulation of inositol monophosphate (IP1) in the frontal cortex upon DOI administration showed no sex-related effect in C57BL/6J mice. However, the pharmacokinetic properties of DOI differed among sexes - brain and plasma concentrations of DOI were lower 30 and 60 min after drug administration in female as compared to male C57BL/6J mice. Together, these results suggest strain-dependent and sex-related differences in the behavioral and pharmacokinetic profiles of the 5-HT2AR agonist DOI in C57BL/6J mice, and support the importance of studying sex as a biological variable in preclinical psychedelic research." Read more at the source #DrGPCR #GPCR #IndustryNews

Objective: The goal of this study was to determine the glucometabolic effects of acute activation of Gs signaling Results: Acute stimulation of GsD signaling in SKM impaired glucose tolerance in lean and obese mice The acute metabolic effects of UCN2 were not mediated by SKM Gs signaling. Conclusions: Selective activation of Gs signaling in SKM causes an acute increase in blood glucose levels

Chemical communication controls a wide range of behaviors via conserved signaling networks. In this study, we investigated the role of chemical signaling in axon regeneration in Caenorhabditis Therefore, the ascaroside signaling system provides a unique example of a signaling molecule that regulates However, it remains unclear what signals activate the EGL-30 pathway in axon regeneration. Thus, ascaroside signaling promotes axon regeneration by activating the GPCR-Gqα pathway.

Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in primary Sjögren's First, excessive activation of β-arrestin2 and GRP78-ATF6-CHOP apoptosis signaling were detected in specimens In vivo, we found that inhibition of GRP78-ATF6-CHOP apoptosis signaling improved ESS symptoms, and the indices, and improved tissue integrity in the ESS model by downregulating GRP78-ATF6-CHOP apoptosis signaling In addition, β-arrestin2 depletion downregulated GRP78-ATF6-CHOP apoptosis signaling to alleviate cell

AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP relationship between the conformational change of the receptor because of the mutation and related downstream signaling Their functionality in terms of cAMP production via Gαs protein coupling was decreased compared to the understanding of the relationship between the changed conformation of the receptor and consequently activated signaling

β-arrestin recruiting GPR84 agonists "In order to avoid a prolonged pro-inflammatory neutrophil response, signaling Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination

August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends Although studies have focused on the G-protein signaling state, the mechanism for β-arrestin signaling

GPCR Symposium on GPCR Activation and Signaling held on May 19th, 2023. signalling: Implication for l-Dopa-induced dyskinesia. Neuroscience Arrestin-dependent nuclear export of phosphodiesterase 4D promotes GPCR-induced nuclear cAMP signaling required for learning and memory. Developmental and homeostatic signaling transmitted by the G-protein coupled receptor FPR2.

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

GPCR Activation and Signaling The dual-function chemokine receptor CCR2 drives migration and chemokine Platelet P2Y1 receptor exhibits constitutive G protein signaling and β-arrestin 2 recruitment. Multiple Potassium Channel Tetramerization Domain (KCTD) family members interact with Gβγ, with effects on cAMP signaling. Non-canonical Golgi-compartmentalized Gβγ signaling: mechanisms, functions, and therapeutic targets.

Join us for the first virtual cafe talk to hear about the amazing work that Dr. Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe