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. There are multiple examples of the induction of CCN proteins by LPA, and by the related lipid mediator Specifically, CCNs secreted into the extracellular space can facilitate the activation of additional receptors

< GPCR News < GPCRs in Oncology and Immunology The path of GPR87: from a P2Y-like receptor to its role progression Published date December 6, 2024 Abstract "GPR87 is a G protein-coupled seven-transmembrane receptor first described as an orphan receptor in 2001. Despite its high structural homology to several extracellular nucleotide-activated P2Y receptors and Authors Katrin Sak Tags Carcinogenesis , GPR87 , LPA receptor , Metastasis , Orphan GPCR , P2Y receptor

Published date June 26, 2023 Abstract "The functional association between stimulation of G-protein coupled receptors We also observed PTX-dependent TNT biogenesis in response to lysophosphatidic acid (LPA), indicative TNT generation by either 5-oxo-ETE or LPA is partially dependent on the transactivation of the epidermal growth factor receptor (EGFR) and impaired by PI3K inhibition.

signaling and cell migration Published date September 25, 2023 Abstract "Background: G protein-coupled receptor CXC chemokine receptor 4 (CXCR4) and its ligand CXCL12, both of which are overexpressed in many cancers Likewise, lysophosphatidic acid receptor 1 (LPA1) is implicated in cancer cell proliferation and migration 4 , Chemotaxis , G protein-coupled receptor , GPCR heteromer , GPCR signaling , Inflammatory disease , Lysophosphatidic acid receptor 1 Source Contribute to the GPCR News Coming soon Become a Contributor

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) are the most frequently Our approach was confirmed by re-discovery of established cancer targets such as the LPA and mGlu receptor families, but also discovered novel GPCRs which had not been linked to cancer before such as the P2Y Receptor

Previous studies have identified the pivotal role of Lysophosphatidic acid (LPA)-signaling in ovarian Our earlier transcriptomic analysis identified Urothelial Carcinoma Associated-1 (UCA1) as an LPA-stimulated In this study, we elucidate the tripartite interaction between LPA-signaling, UCA1, and let-7 miRNAs

< GPCR News < GPCRs in Oncology and Immunology Involvement of Protease-Activated Receptor2 Pleckstrin While the involvement of G-protein-coupled receptors (GPCRs) in cancer is growing, GPCR-based therapies Here, we demonstrate the overexpression of protease-activated receptor 2 (PAR2), a GPCR member in the Grisaru-Granovsky , Shunit Armon , Tatyana Rudina , Priyanga Appasamy , Rachel Bar-Shavit Tags G-protein coupled receptors GPCRs) , fallopian tubes (FTs) , ovarian cancer , pleckstrin homology (PH) domain , protease-activated receptors

< GPCR News < GPCRs in Oncology and Immunology The EBI2 receptor is coexpressed with CCR5 in CD4+ T cells 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.

< GPCR News < GPCRs in Oncology and Immunology Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal cancer Published date June ) receptor inhibited the growth of GAL2 receptor-expressing patient-derived xenografts (PDX) of pancreatic with high GAL2 receptor expression. for GAL2 receptor agonists.

< GPCR News < GPCRs in Oncology and Immunology Olfactory Receptors and Tumorigenesis: Implications for Diagnosis and Targeted Therapy Published date October 4, 2024 Abstract "Olfactory receptors (ORs) are a class of G protein-coupled receptors (GPCR) widely distributed in olfactory sensory neurons and various Increasing evidence reveals the heightened expression of olfactory receptors in tumorous tissues and Authors Yi Tang, Ye Tian, Chun-Xia Zhang, Guo-Tai Wang Tags G Protein-coupled receptors , Olfactory receptors

< GPCRs in Oncology and Immunology The Effect of Cancer-Associated Mutations on Ligand Binding and Receptor Function - A Case for the 5-HT2C Receptor Published date October 29, 2024 Abstract "The serotonin 5- HT2C receptor is a G protein-coupled receptor (GPCR) mainly expressed in the central nervous system. In this study, we aimed to investigate the effects of cancer patient-derived 5-HT2C receptor mutations on ligand binding and receptor functionality.

< GPCR News < GPCRs in Oncology and Immunology G protein-coupled estrogen receptor (GPER)/GPR30 forms a complex with the β1-adrenergic receptor, a membrane-associated guanylate kinase (MAGUK) scaffold protein 30 (GPR30), also named G protein-coupled estrogen receptor (GPER), and the β1-adrenergic receptor (β1AR ) are G protein-coupled receptors (GPCR) that are implicated in breast cancer progression. Both receptors contain PSD-95/Discs-large/ZO-1 homology (PDZ) motifs in their C-terminal tails through

< GPCR News < GPCRs in Oncology and Immunology Signaling by Neutrophil G Protein-Coupled Receptors that Neutrophils, which express many receptors that are members of the large family of G protein-coupled receptors (FPRs) and free fatty acids recognized by free fatty acid receptors (FFARs) regulate neutrophil functions The activation profiles of these receptors include the release of reactive oxygen species (ROS) generated The receptors have signaling and functional similarities, although there are also important differences

< GPCR News < GPCRs in Oncology and Immunology From odor to oncology: non-canonical odorant receptors in cancer Published date December 12, 2023 Abstract "Odorant receptors, traditionally associated with Alongside the canonical GPCR odorant receptors, dysregulation of non-canonical odorant receptors such as trace amine-associated receptors (TAARs), formyl peptide receptors (FPRs), and membrane-spanning The roles of these non-canonical chemoreceptors in cancer are complex, with some receptors promoting

Sponsors GPCR Retreat Program < Back to schedule Atypical Structure and Function of Typical Chemokine Receptors of the principal efforts of our laboratory is to understand the physiological consequences of NMDA receptor The NMDA receptor is a subtype of glutamate neurotransmitter receptor that regulates the formation and Our laboratory is interested in the role of NMDA receptors not only on neurons, but also on other cells Our laboratory has a long-standing interest in the way that NMDA receptors contribute to the symptoms

GPCRs in Oncology and Immunology [1,2,4]Triazolo[1,5-c]pyrimidines as Tools to Investigate A3 Adenosine Receptors in Cancer Cell Lines Published date September 7, 2023 Abstract "A3 adenosine receptor is an interesting [1,2,4]triazolo[1,5-c]pyrimidines has been carried out, obtaining potent and selective A3 adenosine receptor and A1 and A2A adenosine receptors. Compound 20 has been tested on both A3 adenosine receptor positive cancer cell lines (CHO-A3AR transfected

GPCR News < GPCRs in Oncology and Immunology Expression prevalence and dynamics of GPCR somatostatin receptors NET: a paired immunohistochemistry approach Published date November 27, 2023 Abstract "Somatostatin receptors Among the five somatostatin receptors, SST2 and SST3 are associated with apoptosis and cell cycle arrest , making these receptor subtypes better differentiated targets in precision oncology. The expression prevalence of both receptors tends to decline with tumor progression.

< GPCR News < GPCRs in Oncology and Immunology Chemoattractant receptor signaling in humoral immunity on orchestrated migration of B cells within lymphoid organs, which is governed by G protein-coupled receptors ligand binding, GPCRs are phosphorylated by different GPCR kinases (GRKs) at distinct sites on the receptor C termini, which dictates functional outcomes of β-arrestin-mediated signaling, ranging from receptor In this review, we summarize the current understanding of chemoattractant receptor signaling in the context

< GPCR News < GPCRs in Oncology and Immunology Stimulation of ectopically expressed muscarinic receptors activation of pAKT pathways in primary T cells Published date June 12, 2023 Abstract "T cell antigen receptor Here, we demonstrate that stimulating G-protein-coupled muscarinic receptors (M1 and synthetic hM3Dq) , suggesting a selective inhibitory effect of muscarinic receptor costimulation. Tags GPCR; T cells; muscarinic receptor; 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) On average, the white cells studied expressed 160 receptor mRNAs (range, 123-206). Some, but far from all, of the receptors we found have been detected earlier. We believe our data should stimulate studies of receptor function and contribute to drug development.

Immunology Identification of Small-Molecule Antagonists Targeting the Growth Hormone Releasing Hormone Receptor (GHRHR) Published date August 29, 2024 Abstract "The growth hormone-releasing hormone receptor (GHRHR ) belongs to Class B1 of G protein-coupled receptors (GPCRs). model, where first the C-terminal region of the peptide interacts with the extracellular domain of the receptor and, subsequently, the N-terminus interacts with the seven transmembrane domain of the receptor, resulting

, GPCR , Group 2 innate lymphoid cell , HES , High-affinity Fc receptor for IgE , Hypereosinophilic alpha P , Interleukin-13 receptor , Interleukin-13 receptor alpha 1/2 , Interleukin-31 receptor , Interleukin -31 receptor A , Interleukin-33 receptor , Interleukin-4 receptor alpha , Interleukin-5 receptor alpha 11 , Mas-related family of G protein-coupled receptor X1 , Mas-related family of G-protein-coupled receptor , Transient receptor potential , Transient receptor potential ankyrin 1 , Transient receptor potential

Specifically, I am interested in understanding dysregulated G-protein coupled receptor (GPCR) signaling During my post-doctoral research, I was part of a study that identified the receptors of a novel human In this study, I discovered adrenergic receptors (α2A, α2B, and β2-adrenergic receptors) that serve as the gut microbial metabolite (PAG) receptor and characterized the receptor-metabolite interaction. My long-term plan is to conduct research in the field of receptor biology, with a focus on GPCRs.

< GPCR News < GPCRs in Oncology and Immunology Combinatorial depletions of G-protein coupled receptor pleiotropic and cell type-specific functions Published date November 1, 2022 Abstract G-protein coupled receptor kinases (GRKs) participate in the regulation of chemokine receptors by mediating receptor desensitization They can be recruited to agonist-activated G-protein coupled receptors (GPCRs) and phosphorylate their intracellular parts, which eventually blocks signal propagation and often induces receptor internalization

< GPCR News < GPCRs in Oncology and Immunology The β2-adrenergic receptor associates with CXCR4 multimers Published date April 2, 2024 Abstract "While the existence and functional role of class C G-protein-coupled receptors of consensus is largely due to the inherent challenges of demonstrating the presence of multimeric receptor The C-X-C motif chemokine receptor 4 (CXCR4) is a class A GPCR that is a promising target of anticancer Using a bimolecular fluorescence complementation (BiFC) assay, we identified the β2 adrenergic receptor

< GPCR News < GPCRs in Oncology and Immunology Orphan receptor GPR50 attenuates inflammation and insulin G protein-coupled receptors (GPCRs) are involved in endocrine and metabolic processes as well as many GPR50 (G protein-coupled receptor 50) is an orphan GPCR that shares the highest sequence homology with melatonin receptors. deficiency increased inflammation in 3T3-L1 cells and induced the phosphorylation of AKT and insulin receptor

The team’s projects are devoted to the activation/function of CXCR4-ACKR3 (CXCR7) receptors of the CXCL12 In particular, FB contributed to the discovery that CXCL12 is the ligand for the CXCR4 receptor and can FB’ team has identified the orphan CXCR7/ACKR3 receptor as being the 2nd receptor for CXCL12, which behaves that are categorized into a large subgroup of G protein–coupled (GPCR) leukocyte chemotactic receptors (including CXCR4), and a smaller subgroup of atypical chemokine receptors (including the CXCR7/ACKR3

1, 2022 Abstract Chemokines are chemotactic cytokines whose canonical functions govern movement of receptor Chemokines are a physiologic system that is finely tuned by ligand and receptor expression, ligand or receptor oligomerization, redundancy, expression of atypical receptors and non-GPCR binding partners In cancer, chemokines play paradoxical roles in both the directed emigration of metastatic, receptor-expressing Authors Donovan Drouillard, Brian T Craig, Michael B Dwinell Tags Chemokine receptor; cell migration;