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

Adhesion GPCRs GPR56 C-terminal fragment mediates signal received by N-terminal fragment of another adhesion FFAR4 improves the senescence of tubular epithelial cells by AMPK/SirT3 signaling in acute kidney injury Mechanisms underlying divergent relationships between Ca2+ and YAP/TAZ signaling. Call for GPCR Papers GPCRs: Signal Transduction Advances in Computational and Chemical Methods to study GPCR Signal Transduction.

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

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 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,

GPCR Activation and Signaling Targeting GRK2 and GRK5 for treating chronic degenerative diseases: Advances and future perspectives Non-canonical Golgi-compartmentalized Gβγ signaling: mechanisms, functions, appointment of immuno-oncology experts More millions roll in for Sosei Heptares Call for GPCR Papers GPCRs: Signal Transduction.

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

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

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

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

GPCR Symposium on GPCR Activation and Signaling, May 19th, 2023. GPCR Activation and Signaling How can we improve the measurement of receptor signaling bias? Phosphorylation barcodes direct biased chemokine signaling at CXCR3. The relaxin receptor RXFP1 signals through a mechanism of autoinhibition. Subcellular location defines GPCR signal transduction.

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 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

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

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 study distinguishes between driver residues , which directly influence signal transduction, and modulator efficacy while minimising adverse effects, improving treatment outcomes for conditions influenced by β2AR signalling By pinpointing the molecular determinants of ligand efficacy and potency in GPCR signalling, this research These insights have the potential to advance the treatment of various diseases involving GPCR signalling Molecular determinants of ligand efficacy and potency in GPCR signaling.

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.

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

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

GPCR Activation and Signaling Molecular Mechanisms of PTH/PTHrP class B GPCR Signaling and Pharmacological women blazing trails in biopharma R&D ERNEST - 2022 Scientific Outputs Call for GPCR Papers GPCRs: Signal Transduction.

GPCR Activation and Signaling A multi-dimensional view of context-dependent G protein-coupled receptor Molecular Modeling Study of a Receptor-Orthosteric Ligand-Allosteric Modulator Signaling Complex. GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. therapeutics Sosei Heptares Webinar Presentation for FY2022 Financial Results Call for GPCR Papers GPCRs: Signal Transduction.

GPCR Activation and Signaling New simulation insights on the structural transition mechanism of Bovine GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed Cryo-EM structures of orphan GPR21 signaling complexes. The molecular associations in clathrin-coated pit regulate β-arrestin-mediated MAPK signaling downstream Transduction.

Further investigation of the signaling pathways downstream of GPR183 is needed to support the development GPR183-induced mechano-allodynia was associated with significant activation of MAPKs (extracellular signal-regulated Our findings provide novel mechanistic insight into how GPR183 signaling in the spinal cord produces We found that 7α,25-OHC-induced allodynia is dependent on MAPK and NF-κB signaling pathways and results This study provides a first insight into how GPR183 signaling in the spinal cord is pronociceptive."

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