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

At the cellular level, the plasmatic membrane is a thin layer of lipids that surrounds the entire cell interplay between GPCRs and β-arrestins and how this complex operates on the plasma membrane of living cells dissected the sequence of events in receptor-β-arrestin interactions at the plasma membrane of living cells Cell, 186(10), 2238–2255.e20. https://doi.org/10.1016/j.cell.2023.04.018 Janetzko, J., Kise, R., Barsi-Rhyne Cell, 185(24), 4560–4573.e19. https://doi.org/10.1016/j.cell.2022.10.018 Latorraca, N.R., Wang, J.K.,

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

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 However, KP-10 stimulation induced migration of MDA-MB-231, but not BT-20 cells, in a calcium-dependent Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression.

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 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.

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

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

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 receptor-B2 (MRGPRB2), plays important roles in immune response. indicated the involvement of the PLC-IP3-ORAI signaling pathway and CACCS in MRGPRB2-mediated mast cell

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

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

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In addition, one aim is to bring together the mode of action of autoantibodies in immune regulation and

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.

Inhibition of autophagy by 3-methyladenine or interference of ATG5 or ATG7 attenuated HBx-induced cell

The immune system depends on chemokines to direct cell migration during immune surveillance and inflammation CCR2 is an example of a dual-function receptor that directly regulates both cell migration and scavenging Scavenging allows cells to continuously migrate by remaining responsive to chemokines, it dampens the , and CCR5 switch purely to scavenging (D'Amico G. et al. 2000), becoming incapable of promoting cell migration, a phenomenon which is likely to be mediated by changes in the cell motility machinery with

GPR125 (ADGRA3), an orphan adhesion GPCR, has been shown to modulate planar cell polarity in gastrulating zebrafish, but its biochemical properties and role in mammalian cells have remained largely unknown. and human embryonic kidney HEK293 cells. Furthermore, in polarized MDCK cells, GPR125 is exclusively recruited to the basolateral domain of the in Matrigel 3D culture of MDCK cells.