< 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. Joshua Chiou , Sanju Sinha , Marin Matic , Francesco Raimondi , Thomas S Hoang , Rebecca Berdeaux , Dario A A Vignali , Ramiro Iglesias-Bartolome , Hannah Carter , Eytan Ruppin , Jill P Mesirov , J Silvio Gutkind

< GPCR News < GPCRs in Oncology and Immunology Chemoattractant receptor signaling in humoral immunity distinct sites on the receptor C termini, which dictates functional outcomes of β-arrestin-mediated signaling In this review, we summarize the current understanding of chemoattractant receptor signaling in the context in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling

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 Potent inhibitors of ADO signaling are currently being tested in cancer patients, including in randomized I will present our recent work on adenosine-producing ectonucleotidases and adenosine signaling and discuss

< GPCR News < GPCRs in Oncology and Immunology The landscape of cancer-rewired GPCR signaling axes Published , 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

Sponsors GPCR Retreat Program < Back to schedule Biochemical Mechanisms Underlying Location Bias in GPCR Signaling His lab is also interested in identifying novel signal transduction mechanisms of GPCRs, such as the

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

Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Distinct sub-cellular signal Since 2001, he holds the Canada Research Chair in Signal Transduction and Molecular Pharmacology. He is a world-renowned expert in the field of cell signaling and GPCRs and made seminal contributions In addition to paradigm shifts including inverse agonism, biased signaling, and pharmacological chaperones

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."

< 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

< 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

Contest Committee Sponsors GPCR Retreat Program < Back to schedule Inhibition of Relaxin Autocrine Signaling Rottapel’s research interests lies in the elucidation of signal transduction pathways in cancer, immune

< 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 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."

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

< 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

< 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

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 Dynamic Phosphoproteomics of BRS3 Activation Reveals the Hippo Signaling this study, a quantitative phosphoproteomics approach was employed to comprehensively decipher the signal analysis revealed that 27 phosphopeptides corresponding to six proteins were involved in the Hippo signaling Verification experiments demonstrated that downregulation of the Hippo signaling pathway caused by BRS3 demonstrate that BRS3 activation contributes to cell migration through downregulation of the Hippo 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

News < GPCRs in Oncology and Immunology LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling Background: G protein-coupled receptor heteromerization is believed to exert dynamic regulatory impact on signal In contrast, CXCR4 had no impact on LPA1-mediated signaling. Conversely, CXCL12-induced calcium signaling and migration were increased in LPAR1 knockout cells, and LPA1-selective antagonists enhanced CXCL12-induced Gαi/o signaling and cell migration in the parental

Oncology and Immunology From outside to inside and back again: the lysophosphatidic acid-CCN axis in signal CCN proteins act to facilitate signaling events involving extracellular matrix proteins. The signaling pathways responsible for LPA/S1P-induced CCN1/2 typically involve activation of the small Inducible CCNs can potentially play roles in downstream signal transduction events required for LPA and In this way, an extracellular signal (LPA or S1P) can activate GPCR-mediated intracellular 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

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.

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 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

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.

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

< 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