< GPCR News < GPCRs in Oncology and Immunology G Protein-coupled Receptor-mediated Membrane Targeting protein-coupled receptors (GPCRs) activate β phospholipase C (PLCβ) while receptor tyrosine kinases ( The study reveals a molecular mechanism of membrane targeting of PLCγ2 and the signaling pathways by Tags G protein-coupled receptor (GPCR) , calcium-promoted Ras inactivator (CAPRI) , chemotaxis , neutrophils in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology Activation of PI3K/Akt pathway by G protein-coupled receptor Among eukaryotes, the G protein-coupled receptor (GPCR) family stands as the largest group of membrane proteins. As a member of the GPCR family, G protein-coupled receptor 37 (GPR37) exhibits unknown functions in tumors elevated GPR37 expression predicts an unfavorable prognosis. (2) It was demonstrated that GPR37 positively regulates

News < GPCRs in Oncology and Immunology Blockade of vasoactive intestinal peptide receptor 2 (VIPR2) signaling protein-coupled receptor that binds to Gαs, Gαi, and Gαq proteins to regulate various downstream signaling molecules, such as protein kinase A (PKA), phosphatidylinositol 3-kinase (PI3K), and phospholipase C KS-133 in the presence of VIP decreased the phosphorylation of extracellular signal-regulated kinase Our findings suggest that VIPR2 signaling regulates cyclin D1 levels through the cAMP/PKA/ERK and PI3K

< GPCR News < GPCRs in Oncology and Immunology [Inhibitory effect of downregulating G protein-coupled expression levels of the inflammatory cytokines in GFs induced by LPS, namely, interleukin (IL)-1β, IL-6, group (0.004±0.000, 0.004±0.000, 0.002±0.000, 0.007±0.000) (all P<0.001), respectively, and peaked at 6 RT-qPCR results showed that the expressions of IL-8, IL-1β, IL-6, TNF-α, and PTGS2 at the gene level Moreover, GPRC5A played a role in inflammation regulation by interacting with NF-κB signaling pathway

protein-coupled receptor with the neuropeptide VIP as a ligand. Overexpressed VIPR2 caused increases in the levels of cAMP and phosphorylated extracellular signal-regulated kinase (ERK), which involves a VIPR2 signaling pathway through Gs protein. Moreover, an inhibitor of mitogen-activated protein kinase kinase, U0126, attenuated tumor proliferation Together, these findings suggest that VIPR2 controls breast tumor growth by regulating the cAMP/PKA/ERK

< GPCR News < GPCRs in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 G protein-coupled receptors (GPCRs) activated by limited n-terminal proteolysis. PARs are highly expressed in many cancer cells, including prostate cancer (PCa), and regulate various through this autocrine signaling mechanism. Overall, these results demonstrate that autocrine signaling through PARs is an important regulator of

Caron at Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking , and signaling. His research career has focused on the investigation of the regulation of G protein-coupled receptors signaling mechanisms in health and disease.

pathways and trafficking Localization of putative ligands for adhesion G protein-coupled receptors in Pal Kasturi Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues G-protein signaling by binding to extracellular matrix proteins and mechanotransduction. GPCR signaling and trafficking can be regulated by several different post-translational modifications signalling.

Caron at Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking , and signaling. His research career has focused on the investigation of the regulation of G protein-coupled receptors signaling mechanisms in health and disease.

Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Targeting adenosine signaling for immuno-oncology Date & Time Friday, November 3rd / 4:35 PM Abstract "Adenosine (ADO) signaling through A2A and A2B G protein-coupled receptors is increasingly recognized as an important immune checkpoint Potent inhibitors of ADO signaling are currently being tested in cancer patients, including in randomized unexpected links between the adenosinergic pathway, DNA damage response and metabolic regulation."

< GPCR News < GPCRs in Oncology and Immunology The GPCR adaptor protein Norbin controls the trafficking neutrophils Published date October 28, 2024 Abstract "Norbin (Neurochondrin, NCDN) is a GPCR adaptor protein their steady state trafficking and sometimes their agonist-induced internalisation, as well as their signalling CXCR4 function in neutrophils and increases our understanding of the mechanisms through which Norbin regulates Authors Stephen A Chetwynd, Richard J Ward, Graeme Milligan, Heidi C E Welch Tags C5aR1 , CXCR4 , G protein-coupled

homeostasis is altered by the tumor microenvironment Published date November 20, 2023 Abstract " Background: Regulator of G protein signaling 5 (RGS5), as a negative regulator of G protein-coupled receptor (GPCR) signaling Zhang , Xiao-Fu Huang , Yu Song , Wen-Di Zhang , Rui-Juan Guo , Han Li , Mei Han Tags Breast cancer , Regulator of G protein signaling 5 , Vascular remodeling , Vascular smooth muscle cells Source Contribute to the in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

compact multidomain module of fourteen domains which regulates signaling Sumit Bandekar Unveiling the hallmark feature of adhe-sion G-protein coupled receptors (ADGRs), as this extracellular domain contains signaling Sumit Bandekar Abstract "Cadherin EGF Laminin G seven-pass G-type receptors (CELSRs) are conserved adhesion G protein-coupled receptors; they are essential for embryogenesis and neural development. signaling.

transduction Published date September 1, 2023 Abstract "CCN1 and CCN2 are matricellular proteins that CCN proteins act to facilitate signaling events involving extracellular matrix proteins. Lysophosphatidic acid (LPA) is a lipid that activates G protein-coupled receptors (GPCRs), enhancing GTP-binding protein Rho and the transcription factor YAP. In this way, an extracellular signal (LPA or S1P) can activate GPCR-mediated intracellular signaling

< GPCR News < GPCRs in Oncology and Immunology G protein-coupled receptors related to autoimmunity in In particular, the association of the disease with several types of anti-G protein-coupled receptor ( Authors Yoko Sunami, Keizo Sugaya, Kazushi Takahashi Tags G protein-coupled receptors , Autoimmunity in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology G protein coupled receptor transcripts in human immune cells and platelets Published date September 27, 2024 Abstract "G-protein coupled receptors (GPCRs) Platelets made 69. Some, but far from all, of the receptors we found have been detected earlier. in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

in Adhesion G Protein-Coupled Receptors Cheng-Chih Hsiao ADGRG1/GPR56 regulates survival of terminally in Axons Monserrat Avila Zozaya The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial Activity In The G12/13 Pathway Nicole Perry-Hauser Adhesion G protein-coupled receptor latrophilin-3 protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in protein-coupled receptors in mouse tissues.

< GPCR News < GPCRs in Oncology and Immunology Chemokine N-terminal-derived peptides differentially regulate elevated in disease settings, where the largest group of CC-chemokines are the macrophage inflammatory proteins MIP chemokines, such as CCL3 and CCL5 are processed at the N-terminus, which influences signaling in Here, we investigate the signaling capacity of peptides corresponding to truncated N-termini. modulator boosting the signal of several chemokine variants on CCR5.

Elva moved to Canada where she obtained her Ph.D. at the University of Western Ontario, working on the regulation of G proteins signaling by accessory proteins, such as RGS proteins and GPSM proteins. Her current research focuses on class B GPCRs and understanding how GPCR signaling and function is mediated

In addition to contributing to energetic and biosynthetic demands, metabolites can also function as signaling This metabolite binds to and regulates the function of diverse proteins intracellularly to influence metabolism, oxidative response, epigenetic modification, and gene expression and to signal extracellularly through binding the G protein-coupled receptor (GPCR). In this article, we review ITA metabolism and its regulation, discuss its target proteins and mechanisms

< GPCR News < GPCRs in Oncology and Immunology Chemoattractant receptor signaling in humoral immunity protein-coupled receptors (GPCRs) responding to chemoattractants, represented by chemokines. distinct sites on the receptor C termini, which dictates functional outcomes of β-arrestin-mediated signaling Our recent study revealed that a protein complex consisting of copper metabolism MURR1 domain-containing In this review, we summarize the current understanding of chemoattractant receptor signaling in the context

< GPCR News < GPCRs in Oncology and Immunology Stretch regulates alveologenesis and homeostasis via mesenchymal Published date April 27, 2023 Abstract " Alveolar development and repair require tight spatiotemporal regulation of numerous signalling pathways that are influenced by chemical and mechanical stimuli. Transforming growth factor-β (TGFβ) is essential for alveologenesis and lung repair, and the G protein Cyclical mechanical stretch-induced TGFβ activation required Gαq/11 signalling and serine protease activity

and cell migration Published date September 25, 2023 Abstract "Background: G protein-coupled receptor heteromerization is believed to exert dynamic regulatory impact on signal transduction. protein activation, β-arrestin recruitment, ligand binding, and transwell migration assays. In contrast, CXCR4 had no impact on LPA1-mediated signaling. protein-coupled receptor , GPCR heteromer , GPCR signaling , Inflammatory disease , Lysophosphatidic

< GPCR News < GPCRs in Oncology and Immunology The landscape of cancer-rewired GPCR signaling axes Published date May 8, 2024 Abstract "We explored the dysregulation of G-protein-coupled receptor (GPCR) ligand Multiple GPCRs are differentially regulated together with their upstream partners across cancer subtypes , cancer , cancer cell lines , cell-cell communication , drug repurposing , personalized medicine , signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology Context-dependent ciliary regulation of hedgehog pathway regulates mesoscale organization of tissues. We studied hedgehog pathway repression by the GPCR GPR161, and the ankyrin repeat protein ANKMY2 that direct cAMP/protein kinase-A signaling by cilia in GLI-R generation. that is cAMP signaling competent.

GPCR News < GPCRs in Oncology and Immunology Pan-cancer functional analysis of somatic mutations in G protein-coupled receptors Published date December 1, 2022 Abstract G Protein-coupled receptors (GPCRs While the location of the mutations across the protein domains did not differ significantly in the two in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

axis Published date August 15, 2023 Abstract "The G protein-coupled receptor (GPCR) US28 encoded by AKT and CHK1 and the transcriptional regulators cMYC and STAT3 and by increasing the abundance of cancerous inhibitor of PP2A (CIP2A), driving several feed-forward signaling loops. Inhibition of S1P signaling abrogated the proliferative and anti-apoptotic effects of US28. US28 also activated the S1P signaling axis in HCMV-infected cells.

and Immunology NPFF stimulates human ovarian cancer cell invasion by upregulating MMP-9 via ERK1/2 signaling NPFF regulates a variety of physiological functions by binding to a G protein-coupled receptor (GPCR) The pathogenesis of EOC can be regulated by many local factors, including neuropeptides, through an autocrine Our results also showed that ERK1/2 signaling was activated in SKOV3 cells in response to the NPFF treatment In addition, blocking the activation of ERK1/2 signaling abolished the NPFF-induced MMP-9 expression