Committee Sponsors GPCR Retreat Program < Back to schedule Unveiling Non-Canonical Functions for Gαq Signaling During this period and her doctoral thesis, she has deepened the regulatory mechanisms of GPCR signaling characterization of proteins that act at the level of G proteins and which are part of a multimolecular signaling complex (AGS, de “Activators of G-protein signaling). Ribas has characterized the existence of a new signaling pathway with a relevant role in cardiac hypertrophy

< GPCR News < GPCRs in Oncology and Immunology GPR56 signaling pathway network and its dynamics in the Despite its important role in cancer, its mechanism of action or signaling is not completely understood , growth factors, and inflammation signaling pathways. Here we present a curated signaling map of GPR56 in the context of GBM and discuss the relevance and GPR56 signaling and mesenchymal transition."

< GPCR News < GPCRs in Oncology and Immunology Regulator of G protein signaling 16 restrains apoptosis in colorectal cancer through disrupting TRAF6-TAB2-TAK1-JNK/p38 MAPK signaling Published date June 21 G protein signaling (RGS) protein family modulators play essential role within regulating downstream signaling of GPCR receptors, with function in cancers unclear. study focused on the expression patterns of RGS proteins in CRC, identifying Regulator of G protein signaling

Contest Committee Sponsors GPCR Retreat Program < Back to schedule Using food perception and bioamine signaling laboratory focuses on how organisms perceive and respond to environmental stress though cell non autonomous signaling mechanisms, and how these signals affect the health and longevity of the animal."

GPCRs in Oncology and Immunology Small-molecule targeting of GPCR-independent noncanonical G-protein signaling 11, a first-in-class small-molecule inhibitor of noncanonical activation of heterotrimeric G-protein signaling Gαi) specifically disrupted their engagement with GIV/Girdin, thereby blocking noncanonical G-protein signaling In contrast, IGGi-11 did not interfere with canonical G-protein signaling mechanisms triggered by GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

News < GPCRs in Oncology and Immunology Chemokine N-terminal-derived peptides differentially regulate signaling 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. These 3 to 10-residue peptides displayed weak potency but, surprisingly, retained their signaling on modulator boosting the signal of several chemokine variants on CCR5.

< GPCR News < GPCRs in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 biosensors, we showed that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling Overall, these results demonstrate that autocrine signaling through PARs is an important regulator of in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology Signaling by Neutrophil G Protein-Coupled Receptors that phagocytes are rapidly recruited from the bloodstream to inflamed tissues by chemotactic factors that signal Danger-signaling molecular patterns such as the N-formylated peptides that are formed during bacterial The receptors have signaling and functional similarities, although there are also important differences in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

Immunology A virally encoded GPCR drives glioblastoma through feed-forward activation of the SK1-S1P1 signaling Here, we showed that US28 increased the malignancy of U251 glioblastoma cells by enhancing signaling US28 expression increased the abundance of the key components of the S1P signaling axis, including an Inhibition of S1P signaling abrogated the proliferative and anti-apoptotic effects of US28. US28 also activated the S1P signaling axis in HCMV-infected cells.

< GPCR News < GPCRs in Oncology and Immunology G protein-coupled receptor-mediated signaling of immunomodulation Here, we discuss the current understanding of the roles of GPCRs and their signaling pathways in tumor in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

GPCR News < GPCRs in Oncology and Immunology Orphan receptor GPR50 attenuates inflammation and insulin signaling These data suggest that GPR50 can attenuate inflammatory levels and regulate insulin signaling in adipocytes Furthermore, the effects are mediated through the regulation of the IRS1/AKT signaling pathway and PPAR-γ Weicong Qiu, Cairong Li, Jian V Zhang, Pei-Gen Ren Tags Diabetes mellitus type 2; GPR50; IRS1; Insulin signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology Systems modeling of oncogenic G-protein and GPCR signaling Mathematical models of biochemical reaction networks are an important and emerging tool for the study of cell signaling the present study, we first develop a mechanistic mathematical model of a G-protein coupled receptor signaling hypothesize that CYSLTR2 mutations in UM must co-occur with other mutations to activate FAK/YAP/TAZ signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology GPCR signaling contributes to immune characteristics of multi-omics analysis of NKTCL revealed that EBV gene pattern correlated with immune-related oncogenic signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

non-small cell lung carcinoma proliferation via autophagy activation and inhibition of the PKA-Hippo signaling Regulator of G protein signaling 20 (RGS20) is identified as an upregulated factor in many cancers, yet Western blotting demonstrated different expressions of autophagy and the Hippo-PKA signal pathway. Transcriptomic sequencing suggested the involvement of the Hippo signaling pathway in the action of RGS20 Remarkably, inhibiting Hippo signaling with GA-017 promoted cell proliferation and activated autophagy

inhibition of neuropeptide Y receptors Y1 and Y5 reduces hypoxic breast cancer migration, proliferation, and signaling effects of NPY1R and NPY5R antagonists in normoxia and hypoxia on migration, proliferation, invasion, and signaling Antagonizing NPY1R and/or NPY5R in hypoxia compared to normoxia more greatly reduced MAPK signaling, oxygen availability, therefore further investigations are required to dissect the intricacies of NPYR signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

and Immunology NPFF stimulates human ovarian cancer cell invasion by upregulating MMP-9 via ERK1/2 signaling 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 NPFF stimulates EOC cell invasion by upregulating MMP-9 expression through the NPFFR2-mediated ERK1/2 signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology The GPCR-Gαs-PKA signaling axis promotes T cell dysfunction transgenic mice expressing a chemogenetic CD8-restricted Gαs-DREADD to activate CD8-restricted Gαs signaling and show that a Gαs-PKA signaling axis promotes CD8+ T cell dysfunction and immunotherapy failure. in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology Regulator of G protein signaling protein 6 alleviates Regulator of G protein signaling protein 6 (RGS6), identified as a tumor suppressor gene, has received The RGS6 overexpression plasmid was constructed for transfection. qRT‒PCR was used to assess proinflammatory Yuanlin Song Tags Acute lung injury , Apoptosis , Cell-renewal , Inflammation , Regulator of G protein signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes 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. Together, these findings suggest that VIPR2 controls breast tumor growth by regulating the cAMP/PKA/ERK signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology S1P Signaling Genes as Prominent Drivers of BCR-ABL1-Independent This study investigated the sphingosine-1-phosphate (S1P) signaling-associated genes (SphK1 and S1PRs Their network analysis uncovered significant clusters, emphasizing the interconnectedness of the S1P signaling Moreover, the S1P signaling genes are promising therapeutic targets and plausible new innovation avenues in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

Efferocytes release extracellular vesicles to resolve inflammation and tissue injury via prosaposin-GPR37 signaling macrophage GPR37 to increase expression of the efferocytosis receptor Tim4 via an ERK-AP1-dependent signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology GPR68-ATF4 signaling is a novel prosurvival pathway in Using our small molecule inhibitor OGM and genetic means, we show that blocking GPR68 signaling results Conclusion: These results indicate GPR68 emerges as a critical sensor for an autocrine pro-tumorigenic signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

< GPCR News < GPCRs in Oncology and Immunology DANGER Signals Activate G-Protein Receptor Kinases Suppressing Background: Injury mobilizes primitive 'DANGER signals' (DAMPs) activating innate immunocyte (neutrophils , PMN) signaling and function. Methods: We studied human and mouse PMN signaling elicited by mtDAMPs (GPCR surface expression; protein in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

Immunology Functional Assessment of Cancer-Linked Mutations in Sensitive Regions of Regulators of G Protein Signaling (RGS) proteins modulate G protein-coupled receptor (GPCR) signaling by acting as negative regulators and tolerant RGS14-S127P and RGS10-S64T resulted in a loss-of-function phenotype in GPCR-G protein signaling overlap with cancer-linked mutations cause phenotypic changes that negatively impact GPCR-G protein signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

News < GPCRs in Oncology and Immunology Blockade of vasoactive intestinal peptide receptor 2 (VIPR2) signaling G protein-coupled receptor that binds to Gαs, Gαi, and Gαq proteins to regulate various downstream signaling 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 in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

TIPE proteins control directed migration of human T cells by directing GPCR and lipid second messenger signaling our work describes a new mechanistic paradigm for how human T cells integrate GPCR and phospholipid signaling Goldsmith , Zienab Etwebi , Chin Nien Lee , Youhai H Chen , Honghong Sun Tags Directed migration , PI3K signaling in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

Immunology Natural carboxyterminal truncation of human CXCL10 attenuates glycosaminoglycan binding, CXCR3A signaling resonance for glycosaminoglycan (GAG) binding affinity, assays for cell migration, second messenger signaling Moreover, CXCL10(1-73) exhibited an attenuated capacity to induce CXCR3A-mediated signaling, as evidenced in calcium mobilization assays and through quantification of phosphorylated extracellular signal-regulated : Our study shows that the C-terminal residues Lys74-Pro77 of CXCL10 are important for GAG binding, signaling

Retreat Program < Back to schedule Interaction with the cell adhesion molecule NEGR1 affects mGluR5 cell signalling