Sponsors GPCR Retreat Program < Back to schedule A positive Allosteric Modulator of M1 Acetylcholine Receptors Molecular Medicine and Neuroscience at the University of Ottawa as a Postdoctoral Fellow to explore novel G protein-coupled receptor (GPCR) candidates that can be targeted pharmacologically to slow neurodegeneration

Xu et al. identified the mammalian neurokinin 3 receptor (TACR3), a homolog of the G protein-coupled receptor TkR99D in fruit flies, as a potential therapeutic target for alleviating renal tubular dysfunction

in Oncology and Immunology Phase 1/2 study of sorafenib added to cladribine, high-dose cytarabine, G-CSF , and mitoxantrone in untreated AML Published date September 12, 2023 Abstract "CC chemokine receptor -3 (hCCR3), a G protein-coupled receptor (GPCR) expressed predominantly on eosinophils, is an important This study constructed a nanogold receptor sensor using hCCR3 as the molecular recognition element and This offers a novel approach to quantitatively evaluate chemokine-receptor activation and antagonism

in inflammatory diseases and cancers Published date March 15, 2023 Abstract " C-X-C motif chemokine receptor 2 (CXCR2) is G protein-coupled receptor (GPCR) and plays important roles in various inflammatory diseases Hence, we provide an overview containing the discovery history, protein structure, signaling pathways

With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular

< GPCR News < GPCRs in Oncology and Immunology C5aR2 receptor: The genomic twin of the flamboyant C5aR1 C5a is established to interact with a set of genomically related transmembrane receptors, like C5aR1 The C5aR1 is a classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that tailors immune cell activity potentially through β-arrestins rather than G-proteins. dynamics; protein-protein interactions.

G-protein coupled receptors (GPCRs) are essential for sensing chemokine gradients and directing the movement The TNF-α-induced protein 8-like (TIPE or TNFAIP8L) family of proteins are newly described pilot proteins T Cells deficient in both of these proteins completely lost their directionality. TNFAIP8 interacted with the Gαi subunit of heterotrimeric (α, β, γ) G-proteins whereas TIPE2 bound to , chemoattractant sensing , heterotrimeric G proteins Source Contribute to the GPCR News Coming soon

In her postdoctoral period, she has participated in the identification and 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' group has described a new interaction region in a cellular protein that has turned out to be very Ribas has also described a new protective role of G protein-coupled receptor kinase 2 (GRK2), a known

Interaction Inhibitors with Anticancer Activity Published date October 14, 2024 Abstract "Regulators of G-protein signaling (RGS) are a family of approximately 30 proteins that bind to and deactivate the alpha subunits of G-proteins (Gα) by accelerating their GTP hydrolysis rates, which terminates G-protein coupled receptor Thus, RGS proteins are essential in regulating GPCR signaling, and most members are implicated as critical Regulator of G-protein signaling 2 (RGS2), a member of the R4 family of RGS proteins, is overexpressed

< GPCR News < GPCRs in Oncology and Immunology Aberrant hormone receptors regulate a wide spectrum of endocrine tumors Published date September 23, 2024 Abstract "Aberrant G-protein coupled receptor (GPCR somatotroph tumours; AVPR2, D2DR, and SSTR5 in pituitary corticotroph tumours; GLP1R, GIPR, and somatostatin receptors

for the Treatment of Inflammatory Diseases Published date April 20, 2023 Abstract " The CC chemokine receptor 6 (CCR6) is a G protein-coupled receptor (GPCR) involved in a wide range of biological processes. Th17 cells express the CCR6 receptor and inflammatory cytokines, including IL-17, IL-21 and IL-22, which This review highlights the potential as a therapeutic target of the CCR6 receptor in numerous diseases

< GPCR News < GPCRs in Oncology and Immunology DANGER Signals Activate G-Protein Receptor Kinases Suppressing Mitochondrial (mt) formyl peptides (FP) activate G-protein coupled receptors (GPCR) like FPR1. mtDNA and heme activate toll-like receptors (TLR9, TLR2/4). Methods: We studied human and mouse PMN signaling elicited by mtDAMPs (GPCR surface expression; protein

As a young researcher fascinated by chemokine receptors, molecular pharmacology, drug discovery, and GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the

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 Our group previously reported that LPA induces production of CCN1 protein in human prostate cancer cell In these cells, the mitogenic activity of LPA is mediated by LPA Receptor 1 (LPAR1), a GPCR. Specifically, CCNs secreted into the extracellular space can facilitate the activation of additional receptors

nanobody platform within the research group and used this platform to develop nanobodies targeting viral G protein-coupled receptors with a special focus on the human cytomegalovirus-encoded chemokine receptor in multiple projects where he focuses on the generation of nanobodies against "difficult-to-target" proteins

Reveals the Hippo Signaling Pathway for Cell Migration Published date June 25, 2023 Abstract "Bombesin receptor subtype-3 (BRS3) is an orphan G-protein coupled receptor (GPCR) that is involved in a variety of pathological Harvested cellular proteins were digested and phosphopeptides were enriched by immobilized titanium ( Data analysis revealed that 27 phosphopeptides corresponding to six proteins were involved in the Hippo by BRS3 activation could induce the dephosphorylation and nucleus localization of the Yes-associated protein

< GPCR News < GPCRs in Oncology and Immunology The EBI2 receptor is coexpressed with CCR5 in CD4+ T cells and boosts HIV-1 R5 replication Published date May 21, 2024 Abstract " Objective: CCR5, a G protein-coupled receptor (GPCR), is used by most HIV strains as a coreceptor. HIV-1 entry was quantified with virions harboring β-lactamase fused to the viral protein vpr, early and

human GPRC5D homodimer Published date June 19, 2024 Abstract "GPRC5D is an atypical Class C orphan G protein-coupled receptor. Despite its therapeutic potential, the insufficient understanding regarding of the receptor's structure

rt1-bb1, Oprm1, Zfhx2, Gpr83, and Chrm2) were enriched in pathways related to inhibitory Gi-mediated G protein-coupled receptor (Gi-GPCR) neurons and neuropeptide changes. Progressive neuroinflammation spreads after injury, and neurotransmission through Gi-mediated G protein-coupled receptors in the HPA axis and neuropeptide production by the hypothalamus are inhibited.

< GPCR News < GPCRs in Oncology and Immunology Pharmacological inhibition of neuropeptide Y receptors Neuropeptide Y (NPY) is an abundant neurohormone in human breast carcinomas that acts on a class of G-protein coupled receptors, of which NPY1R and NPY5R are the most highly expressed. that NPY1R and NPY5R mRNA abundance is increased by hypoxia inducible factors, which sensitizes these receptors The estrogen receptor positive MCF7 cells were significantly less invasive in 3D spheres when NPY5R was

My project is investigating a new protein ligand for a GPCR and its potential role in obesity. During his graduate studies, Emile is interested in characterizing novel G protein-coupled receptors GPCR Title: Synapse-Associated Protein 102 and Post-Synaptic Density 95 Differentially Shape Dopamine D1 Receptor Signaling About Bassam Albraidy "My thesis focus on studying the interaction of dopamine D1 receptors scaffolding proteins synapse-associated protein 102 and post-synaptic density 95, and the

for Beta-arrestin signaling in the brain in vivo and has established its importance in D2 dopamine receptors These receptors belong to the super-family of G-protein coupled receptors (GPCR), the major molecular (e.g. lithium) used for bipolar disorder therapy target signaling mechanisms regulated by dopamine receptors The Beaulieu group is presently investigating how cell surface express proteins can act as allosteric These investigations have led to the identification of an RNA binding protein (FXR1P) involved in the

< GPCR News < GPCRs in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells Published date June 29, 2023 Abstract "Proteinase-activated receptors (PARs) are G protein-coupled receptors (GPCRs) activated by limited n-terminal proteolysis.

< GPCR News < GPCRs in Oncology and Immunology Blockade of vasoactive intestinal peptide receptor 2 ( progression in MCF-7 cells Published date March 1, 2024 Abstract "Vasoactive intestinal peptide (VIP) receptor 2 (VIPR2) is a G 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)

90 is a Novel Opioid Receptor Signaling Regulator that can be Targeted to Improve Opioid Therapy Dr. Chris de Graaf September 14, 2021 at 12:00:00 PM Learn More >> Designer G protein-coupled receptors as Scott September 15, 2021 at 8:00:00 PM Learn More >> The challenges of targeting RXFP1, the receptor Innate Proximity: Utilizing the Inherent Physicality of Receptor Interactions for Drug Development Dr Ajay Yekkirala September 16, 2021 at 2:00:00 PM Learn More >> Chaperoning G protein-coupled receptors

By combining experimental data with theory on leukocyte chemotaxis guided by the G protein-coupled receptor (GPCR) CCR7, we demonstrate that in addition to its role as the sensory receptor that steers migration Upon exposure to the CCR7 ligand CCL19, dendritic cells (DCs) effectively internalize the receptor and

fibroblast heterogeneity in fibroblast-associated diseases Published date August 1, 2023 Abstract "G protein-coupled receptors (GPCRs) are the largest and most diverse class of signaling receptors. GPCRs regulate many functions in the human body and have earned the title of "most targeted receptors

Plenary Lecture Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Abstract Only Available for AGPCR24 Attendees About Jin-Peng Sun " Since starting my laboratory in 2011, I has focused on G protein coupled receptors, in particular, the We have identified the receptor subfamily to sense the steroid hormones. progesterone and 17-hydroxyprogesterone membrane receptor are GPR126.