October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist-mediated activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR ADGRF5/GPR116 have not been completely deciphered. We set out to investigate the physiological importance of autocatalytic cleavage upstream of the agonistic peptide sequence, an event necessary for NTF displacement and subsequent receptor activation. To examine this hypothesis, we characterized tethered agonist-mediated activation of GPR116 in vitro and in vivo. A knock-in mouse expressing a non-cleavable GPR116 mutant phenocopies the pulmonary phenotype of GPR116 knock-out mice, demonstrating that tethered agonist-mediated receptor activation is indispensable for function in vivo. Using site-directed mutagenesis and species-swapping approaches, we identified key conserved amino acids for GPR116 activation in the tethered agonist sequence and in extracellular loops 2/3 (ECL2/3). We further highlight residues in transmembrane 7 (TM7) that mediate stronger signaling in mouse versus human GPR116 and recapitulate these findings in a model supporting tethered agonist:ECL2 interactions for GPR116 activation." Read more at the source #DrGPCR #GPCR #IndustryNews

the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well

Data by Arne Hansen et a l has introduced a sensitive method for detecting GPCR mRNAs in human immune cells The study reports that human white blood cells express an average of 160 GPCR mRNAs, ranging from 123 , suggesting a potential role in regulating red blood cell production and offering a novel avenue for Additionally, the study identified unique expression patterns of GPCRs in different immune cell types , including B cells, CD4+ T cells, CD8+ T cells, natural killer (NK) cells, and dendritic cells.

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."

into studies focused on obtaining detailed molecular information in the intracellular context ("in-cell ") or those focused on characterizing molecules or events at the cell surface ("on-cell"). In this review, we outline some key NMR techniques applied for on-cell NMR studies through both solution with cell surface membrane proteins such as G-protein coupled receptors (GPCRs) and receptor tyrosine We also provide a brief survey of the applicability of on-cell NMR approaches to other classes of cell

One suggested theory is that cannabinoids regulate a variety of physiological processes within the cells Murine L6 skeletal muscle cells were used in order to clarify additional possible molecular signaling Skeletal muscle cells have often been used; it is well-documented that they express cannabinoid receptors In the current work, it is demonstrated that skeletal muscle cells exhibit functional expression of CB1 Thus, in skeletal muscle cells, a possible physiological expression of CB1 receptors was identified.

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell They have participated in various cellular processes such as cell proliferation, migration, apoptosis

Here, we provide evidence that activated human T cells express GLP-1R. Analysis of CD4+ T cells activated under T helper (Th) 1, Th2, Th17 and regulatory T (Treg) cell differentiation FoxP3+CD25+CD127- iTreg cells. GLP-1R in human CD4+ T cells. Given the high induction of GLP-1R in human iTreg cells, we hypothesize that GLP-1R+ iTreg cells play

August 2022 TAS2R supports odontoblastic differentiation of human dental pulp stem cells in the inflammatory Background: Inflammatory microenvironment promotes odontoblastic differentiation in human dental pulp stem cells

Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon class of heterotrimeric G proteins, which, in turn, activate signaling pathways that ultimately lead to cell CCR2 is an example of a dual-function receptor that directly regulates both cell migration and scavenging and almost completely lost in the GRK2/3/5/6 KO cells, whereas constitutive receptor internalization Scavenging may allow cells to continuously migrate by remaining responsive to chemokines (S.

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

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

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic In the past, treatment of arthritic B cells with a β2-adrenergic receptor (β2-ADR) agonist has been shown In this study, the expression and signaling of β2-ADR in B cells during collagen-induced arthritis (CIA ) were investigated to provide an explanation of why only B cells from arthritic mice are able to improve Splenic B cells were isolated via magnetic-activated cell sorting (MACS).

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on However, in epithelial cells, OGR1 promotes epithelial to mesenchymal transition (EMT) and inflammation localization and alternative signaling pathways may be responsible for the differential effect of OGR1 in each cell

Information exchange and interpretation is essential in biology and understanding how cells integrate of information-coding molecules into complex orchestrated responses is a major challenge for modern cell biology. In complex organisms, cell to cell communication occurs mostly through neurotransmitters and hormones biology.

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

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

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.,

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell They have participated in various cellular processes such as cell proliferation, migration, apoptosis

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.

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 Therefore, it is imperative to understand the precise molecular mechanism of H2R biology.

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

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 hypothesized that THC and CBD will negatively impact the synthesis of milk proteins and lipids, as well as lipid markers in HC11 cells. 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.

signaling pathway From Structure to Solution: How Structural Biology Informs the Development of Drugs Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Biology - Tectonic Therapeutic PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry behaviors in Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology

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 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.