Arrestins regulate a wide range of signaling events, most notably when bound to active G protein-coupled Among the known effectors recruited by GPCR-bound arrestins are Src family kinases, which regulate cellular modulates Fgr activity with a hallmark bell-shaped concentration-dependence, consistent with a role as a signaling

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel This study, published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 DNAJC13 is crucial to the trafficking of DOR, facilitating its downregulation and influencing cellular signaling pathways essential for pain and anxiety regulation. continues to evolve, this study represents a crucial step toward unraveling the understanding of GPCR regulation

Excited to hear Dr. Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe

DOI elicited more HTR in female as compared to male C57BL/6J mice, a sex-specific exacerbated behavior Volinanserin (or M100907) - a 5-HT2AR antagonist - fully prevented DOI-induced HTR in male and female C57BL/6J monophosphate (IP1) in the frontal cortex upon DOI administration showed no sex-related effect in C57BL/6J min after drug administration in female as compared to male C57BL/6J mice. sex-related differences in the behavioral and pharmacokinetic profiles of the 5-HT2AR agonist DOI in C57BL/6J

2025 | 10th German Pharm-Tox Summit NEW April 1 - 5, 2025 | XXIII GEM Meeting in 2025 NEW April 3 - 6, GPCR signalling: Yet another variant route in a highly complex road map Transactivation of the EGF receptor as a novel desensitization mechanism for G protein-coupled receptors, illustrated by dopamine D2-like Endocrinology, and Taste Adipose tissue in older individuals: a contributing factor to sarcopenia Asprosin regulates in murine brain tissue Regulator of G protein signaling 6 (RGS6) in dopamine neurons promotes EtOH seeking

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 Adrenergic receptors on B cells and intracellular β2-ADR downstream molecules (G protein-coupled receptor kinase 2 (GRK-2), β-Arrestin 2, p38 MAPK, extracellular signal-regulated kinase 1/2 (ERK1/2) and cAMP response element-binding protein (CREB)) were analyzed at different time points in naïve and arthritic

Upon activation, chemokine receptors coupe to the Gαi class of heterotrimeric G proteins, which, in turn to remove them from in vivo sites, while maintaining the responsiveness of canonical G protein–coupled C terminus by G protein receptor kinases (GRKs), specifically GRK2 and GRK3 (A. Removal of G proteins by using CRISPR KO of Gαi (Gαi KO) or KO of all Gα subtypes (Gα_all KO) (M. internalization was partially decreased in GRK2/3 KO cells and almost completely lost in the GRK2/3/5/6

S1P5 is predominantly expressed in nervous and immune systems, regulating the egress of natural killer

September 2022 "T cells are master regulators of the immune response tuning, among others, B cells, macrophages A finely tuned signalling compartmentalization orchestrated in dynamic platforms is an essential requirement several studies have depicted the pivotal role of the cytoskeleton and lipid microdomains in controlling signalling Here, we discuss mechanisms responsible for signalling amplification and compartmentalization in T cell We also take into account the detrimental effect of mutations carried by distinct signalling proteins

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that regulates the cardiovascular system as a vasodepressor. The recently determined structures of B2R have provided molecular insights into the functions and regulation

September 2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS Herein, we further elucidated the intracellular signaling pathways mediating in sea bass GnIH actions and the potential interactions with sea bass kisspeptin (Kiss) signaling. GnIH can interfere with kisspeptin actions by reducing its signaling. Our results provide additional evidence for the understanding of signaling pathways activated by GnIH

October 2022 Design and validation of recombinant protein standards for quantitative Western blot analysis radioligand binding assays with antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR) levels requires the use of purified protein standards containing the Results: Here we generated highly soluble and stable recombinant protein constructs GST-CB1414-472 and

Join us and learn how to quantify your kinetic GPCR signaling from the expert himself: Dr.

Previous research showed that activation of Gq/11 proteins by G-protein coupled receptors has pro-nociceptive properties, suggesting that blockade of Gq/11 signalling could be beneficial for pain control.

This study unveiled a new antifibrotic cGAS/STING signaling pathway that suppresses pathological angiogenesis Meanwhile, cGAS deletion upregulated profibrotic Yes-associated protein (YAP) signaling in endothelial Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717, and a G protein-coupled receptor (GPCR)-based antagonist that blocks the profibrotic activity of endothelial Together, our data support that activation of cGAS/STING signaling mitigates organ fibrosis and suppresses

August 2022 "Bone remodeling is precisely regulated mainly by osteoblasts and osteoclasts. Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, metabolite of DHA, we hypothesized that DHA may inhibit osteoclastogenesis by affecting synaptamide/GPR110 signaling These results suggest that synaptamide/GPR110 signaling negatively regulates osteoclastogenesis.

September 2022 "Yeast use the G-protein–coupled receptor signaling pathway to detect and track the mating The G-protein–coupled receptor pathway is inhibited by the regulator of G-protein signaling (RGS) Sst2 which induces Gα GTPase activity and inactivation of downstream signaling. G-protein signaling activates the MAPK Fus3, which phosphorylates the RGS; however, the role of this Completion of cytokinesis in the presence of pheromone is promoted by the kelch-repeat protein, Kel1

Coordinated transcriptomics and peptidomics of central nervous system identify neuropeptides and their G protein-coupled receptors in the oriental fruit moth Grapholita molesta The oriental fruit moth Grapholita Neuropeptides and their specific receptors (primarily G protein-coupled receptors, GPCRs) regulate multiple Here, we generated a transcriptome of the central nervous system (CNS) of G. molesta. determine physiological functions and pharmacological characterization of neuropeptides and their GPCRs in G.

October 2022 "G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one binding site of endogenous ligands (orthosteric site), allosteric modulators offer new avenues for the regulation

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization , internalization, and signaling. that distal, 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 kinase 1/2 phosphorylation.

The hepatitis B virus X protein (HBx) is involved in the process of hepatocellular carcinoma via the ARRB1 interacted with HBx, and the autophagic core protein MAP1LC3/LC3, a scaffolding protein, was essential 1 light chain 3 beta; MKI67: marker of proliferation Ki-67; MTOR: mechanistic target of rapamycin kinase ; MAPK: mitogen-activated protein kinase; 3-MA: 3-methyladenine; NFKB/NF-κB: nuclear factor kappa B; primary human hepatocytes; RB1: RB transcriptional corepressor 1; SQSTM1/p62: sequestosome 1; STAT: signal

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs) are now thought to use endocytosis to promote cellular cAMP signaling that drives downstream transcription of cAMP-dependent genes. hepatic glucose metabolism via cAMP signaling. Together, these results implicate the endosomal signaling paradigm in metabolic regulation by glucagon

One of the CNVs is located on chromosome 4q13.1 in the region of the gene encoding for adhesion G protein-coupled

Aberrant EBI2 signaling is implicated in inflammatory bowel disease, sclerosis, and infectious disease Here, we report the cryo-EM structures of an EBI2-Gi signaling complex with its endogenous agonist 7α Mutations within the oxysterol binding site and the Gαi interface attenuate G protein signaling and abolish oxysterol-mediated cell migration indicating that G protein signaling directly involves in the oxysterol-EBI2

β-arrestin recruiting GPR84 agonists "In order to avoid a prolonged pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR) has to be rapidly terminated. Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination as well as formyl peptide receptor 2 (FPR2), receptors expressed in neutrophils, play a key role in regulating

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 We show that locally restricted suppression of postsynaptic cAMP levels or of cAMP-dependent protein-kinase 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

September 2022 GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation in macrophages "The putative medium-chain free fatty acid receptor GPR84 is a G protein-coupled

Engineered G protein-coupled receptors (GPCRs) are commonly used in chemogenetics as designer receptors