October 2022 "Study of small molecule binding to live cells provides important information on the characterization Here we developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell This versatile method allows quantitative characterization of ligand binding to cell surface expressed

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well As well, it has not been reported whether the effects of temperature on biosensor activity are reversible We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or Temperature optimization studies were carried out using HEK293H cells transiently transfected with the

September 2022 GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response , such as inhibition of cell proliferation, colony formation, migration, invasion and xenograft tumor growth in nude mice as well as induction of G1-phase cell cycle arrest, and vice versa. Besides, we found that GASP1 knockout obviously improved the response of breast cancer cells to paclitaxel Collectively, this study demonstrates that GASP1 enhances malignant behaviors of breast cancer cells

express multiple ORs, tumor cells associated with the nervous system express a single OR gene type ( In the immune system ORs are expressed in different blood cells where aroma compounds from butter, known proliferation via activation by β-ionone which initiates prostate cancer cell cycle arrest (Jones S. In non-small-cell lung cancer OR2J3 activation induced apoptosis and inhibited cell proliferation and The chimeric antigen receptor T cell therapy could also be a way to target tumor cells expressing ectopic

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on extracellular pH in the progression of pulmonary fibrosis, we sought to identify whether pH mediates other cellular However, in epithelial cells, OGR1 promotes epithelial to mesenchymal transition (EMT) and inflammation We then demonstrate that sub-cellular localization and alternative signaling pathways may be responsible for the differential effect of OGR1 in each cell type.

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell intracellular proteins with many functions which interact directly and indirectly with a wide number of cellular They have participated in various cellular processes such as cell proliferation, migration, apoptosis

September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing chimeras subject to GABAB -dependent endoplasmic reticulum sorting to traffic mutant heterodimers to the cell Transfected HEK-293 cells were assessed for Ca2+o -stimulated Ca2+i mobilization using mutations in either

August 2022 GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates GPR3 was relatively highly expressed in retinal ganglion cells (RGCs).

histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell study, for the first time, we demonstrate the nuclear localization of H2R in lymphatic endothelial cells

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin In KISS1R overexpressing triple-negative breast cancer (TNBC) cells, stimulation has been associated MDA-MB-231 cells are metastatic when implanted in mice while BT-20 are not and remain epithelial-like We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression.

GPR3 After wounding, a G-protein coupled receptor promotes the restoration of tension in epithelial cells glutamatergic neurons GPCRs in Oncology and Immunology TIPE proteins control directed migration of human T cells by directing GPCR and lipid second messenger signaling Methods & Updates in GPCR Research A bioluminescent

mammary gland (MG) undergoes remodeling, which involves alveolar differentiation of mammary epithelial cells and gene and protein expression of major milk protein and lipid synthesizing markers. using the HC11 cells as lipid markers in HC11 cells. Our results demonstrated that THC and CBD reduced cellular viability at concentrations above 30μM and In conclusion, 10μM THC and CBD altered the differentiation of HC11 cells, in part via the CB2 receptor

September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell However, the role of β2-AR in oral cancer is not well identified. significance in relation with the clinicopathological features and overall survival of oral squamous cell

protein signalling using a G protein activation assay and second messenger assay conducted on living cells

September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells IGF-1 receptors and G protein-coupled (GPCR) signaling systems leading to mitogenic signaling in PDAC cells agonist neurotensin induced rapid activation of Src family of tyrosine kinases (SFKs) within PANC-1 cells by FAK phosphorylation at Tyr576/577 and Tyr861, sensitive biomarkers of SFK activity within intact cells and suppessed the growth of MiaPaCa-2 cells xenografted into the flank of nude mice.

September 2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells on basal CRE-luc activity, they significantly decreased forskolin-elicited CRE-luc activity in COS-7 cells Moreover, an evident increase in SRE-luc activity was noticed when COS-7 cells expressing GnIHR were Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor and represent a starting point for the study of interactions with multiple neuroendocrine factors on cell

September 2022 A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under and aggressive primary brain tumor, characterized by its high chemoresistance and the presence of a cell subpopulation that persists under hypoxic niches, called glioblastoma stem-like cells (GSCs). Cell viability was measured by MTS assays. Cell cycle and apoptosis were determined by flow cytometry.

Many cause receptor misfolding and failure to reach the cell surface. Pharmacological chaperones are cell-permeant small molecules that engage nascent mutant GPCRs in the endoplasmic reticulum, stabilizing folding and "rescuing" cell surface expression. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants of certain mutant FSHRs with severely reduced cell surface expression.

October 2022 Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein In this study, we generated and characterized human embryonic kidney 293A (HEK293A) cell lines devoid Additionally, using the Gαq/11 inhibitor YM-254890, GPCR kinase 2 and 3 (GRK2 and GRK3) KO cells, and Our PKC KO cell lines expand the repertoire of KO HEK293A cell lines available to research GPCR pharmacology lines as more specific research tools to investigate PKC-mediated aspects of cell biology."

Using multiplexed single-cell transcriptomics, we analyze human neural precursor cells (hNPCs) from sporadic Additionally, we detect a shortening of PC in PINK1-deficient human cellular and mouse models of familial

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety However, our knowledge of how GPCRs regulate liver metabolism and fibrosis in the different cell types In particular, a better understanding of the role of GPCRs in hepatic stellate cells (HSCs), the primary cells that regulate liver fibrosis, may lead to the development of drugs that can improve hepatic fibrosis

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions β-arrestin2 are key integrated signaling nodes in various biological processes, and both of them regulate cell proliferation and promote cell invasion and migration. This review summarizes the roles of GRK2/β-arrestin2 in immune cell function and focuses on the pathological

possesses both immune and vascular privilege, in part due to its unique repertoire of resident immune cells Corneal nerves produce various neuropeptides that have a wide range of functions on immune cells.

Join us for the first virtual cafe talk to hear about the amazing work that Dr. Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR), known as Mas-related G protein-coupled indicated the involvement of the PLC-IP3-ORAI signaling pathway and CACCS in MRGPRB2-mediated mast cell

various chemokine/chemokine receptor axes in trafficking and oriented locomotion of mesenchymal stem cells Application of mesenchymal stem cells (MSCs) as an emerging approach was recruited forthe treatment of Chemokines are low molecular weight proteins that their functional activities are achieved by binding to the cell Chemokine/chemokine receptor axes play a pivotal role in the recruitment and oriented trafficking of immune cells of MS patients via expression of various chemokine receptors in response to chemokines expressed by cells

Through gene expression analysis in immune and gastrointestinal cells, we show that these isoforms emerge Additionally, we employed optical assays in living cells to thoroughly profile both GPR35 isoforms for

wild type αq by binding to αq-GDP and preventing GDP/GTP exchange, the mechanism of YM inhibition of cellular Treatment of cells with YM failed to inhibit signaling by these PM-restricted αqQ209L.