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

< 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

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

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

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

the past two decades, his lab has published numerous groundbreaking findings shedding light on the signaling Most recently, his lab has made a number of seminal contributions to understanding the signaling, regulation has a special interest in studying disease-associated mutations to human GPCRs that perturb receptor signaling learn more about Randy’s work, hear his insights on the GPCR field, and also hear the story of how he came

< 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 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

< 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

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

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 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 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 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

< 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 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

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

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

faculty position at Duke in Gastroenterology, where he remained until 2018 studying GPCRs and their signaling My research focus is on understanding how distinct cellular signaling pathways interact and are coordinated For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling , and characterizing the role of protein S-nitrosylation as a signaling post-translational modification signaling systems.

faculty position at Duke in Gastroenterology, where he remained until 2018 studying GPCRs and their signaling My research focus is on understanding how distinct cellular signaling pathways interact and are coordinated For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling , and characterizing the role of protein S-nitrosylation as a signaling post-translational modification signaling systems.

faculty position at Duke in Gastroenterology, where he remained until 2018 studying GPCRs and their signaling My research focus is on understanding how distinct cellular signaling pathways interact and are coordinated For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling , and characterizing the role of protein S-nitrosylation as a signaling post-translational modification signaling systems.

faculty position at Duke in Gastroenterology, where he remained until 2018 studying GPCRs and their signaling My research focus is on understanding how distinct cellular signaling pathways interact and are coordinated For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling , and characterizing the role of protein S-nitrosylation as a signaling post-translational modification signaling systems.

It turns out that it was signal transduction, and he worked on the signaling cascades involved in heart His encounter and interest in signaling in the context of GPCRs during his postdoctoral training in Dr Today, John and his team focus on understanding how signal transduction cascades downstream of the opioid receptors work, including the unique organization of chaperone protein Hsp90 modulation of opioid signaling

August 1, 2023 Abstract "G protein-coupled receptors (GPCRs) are the largest and most diverse class of signaling and repair of almost all tissues by responding to the cellular cues via diverse and intricate GPCR signaling This review discusses the dynamic architecture of the GPCRs and their intertwined signaling in pathological fibrosis, cardiac fibrosis, pancreatic fibrosis, hepatic fibrosis, and cancer as opposed to the GPCR signaling Understanding the dynamics of GPCR signaling in fibroblasts with disease progression can help in the

in Jeff Benovic’s laboratory studying the regulation of G protein-coupled receptor trafficking and signaling Adriano’s research has contributed to our understanding of the role that ubiquitin plays in GPCR signaling His lab has shown a role for -arrestins and PTMs in GPCR trafficking and signaling and has leveraged this knowledge to reveal the spatial and temporal requirements for GPCR activation of signaling pathways The ultimate goal of Adriano’s research is to target novel aspects of GPCR signaling for therapeutic