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.

([Ca2+]i), which modulate airway smooth muscle tone; and whether they promote airway smooth muscle cell proliferation. in native human and guinea pig airway smooth muscle and cultured human airway smooth muscle (HASM) cells MT2 agonist ramelteon (10 µM) significantly inhibited forskolin-stimulated cAMP accumulation in HASM cells acetylcholine-stimulated [Ca2+]i increases, stress fiber formation through the MT2 receptor in HASM 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.

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

Using multiplexed single-cell transcriptomics, we analyze human neural precursor cells (hNPCs) from sporadic

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."

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

GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. and more Cytotoxicity-related effects of imidazolium and chlorinated bispyridinium oximes in SH-SY5Y cells in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer cell proliferation by enhancing the ERK pathway. Sherwin Sells 30,000 Shares STALICLA signs agreement with Novartis on neurodevelopmental disorders Call

, is a crucial determinant of cellular responses such as proliferation, differentiation, migration, survival proliferation and survival​, highlighting the pressing need to comprehend and control these pathways Cell Receptor-Mediated Gene Expression. Cells, 10(10), 2509. Volmat, V., & Pouysségur, J. (2001). Biology of the Cell, 93(1‐2), 71-79. Wei, H., Ahn, S., Shenoy, S. K., Karnik, S.

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.

Soluble cyclase-mediated nuclear cAMP synthesis is sufficient for cell proliferation. GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. Generation of Gαi knock-out HEK293 cells illuminates Gαi-coupling diversity of GPCRs. development of cachexia therapeutics Sosei Heptares Webinar Presentation for FY2022 Financial Results Call

Soluble cyclase-mediated nuclear cAMP synthesis is sufficient for cell proliferation. Methods & Updates in GPCR Research Mapping of structural arrangement of cells and collective calcium transients: an integrated framework combining live cell imaging using confocal microscopy and UMAP-assisted Christopher Prior, as CEO and Reports Recent Drug Discovery Highlights Call for GPCR Papers GPCRs: Signal

Sakmar and his team used 'bioluminescence resonance energy transfer to measure cell-surface expression of neurodegenerative diseases GPCRs in Neuroscience Primary cilia control oligodendrocyte precursor cell proliferation in white matter injury via Hedgehog-independent CREB signaling Ciliary localization of Preclinical Data for AI-designed LSD1 and MALT1 Inhibitors at ESMO 2023 Restoring the function of a human cell surface protein in yeast cells Trevena Reports Favorable TRV045 Topline Safety and Tolerability Data

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

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

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

for disease therapy GPCRs in Cardiology, Endocrinology, and Taste Transcriptomic profiling highlights cell proliferation in the progression of experimental pulmonary hypertension in rats Latrophilin-2 mediates Metallo-protease Peptidase M84 from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer cells of the nematode-trapping fungus Arthrobotrys flagrans activates mitochondria and reprograms fungal cells Deuteration as a General Strategy to Enhance Azobenzene-Based Photopharmacology Optical Control of Cell-Surface

RGS4 is expressed in various immune cells, including T cells and B cells, and has been shown to modulate immune cell activation and cytokine production. to T cell activation[6]. While in cancer, RGS proteins are involved in regulating cell proliferation and survival[8]. Cell, 1997. 89(2): p. 251-61. https://pubmed.ncbi.nlm.nih.gov/9108480/ 2.

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

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.

Inhibition of autophagy by 3-methyladenine or interference of ATG5 or ATG7 attenuated HBx-induced cell cycle acceleration and the subsequent proliferative response via the induction of G1/S arrest. lysyl oxidase; MAP1LC3B/LC3: microtubule associated protein 1 light chain 3 beta; MKI67: marker of proliferation

Treatment of cells with YM failed to inhibit signaling by these PM-restricted αqQ209L.

Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism, microbiota, and T cell-induced Here, we show that the gut IEL GLP-1 receptor (GLP-1R) is not required for enteroendocrine L cell GLP anti-inflammatory actions of GLP-1RAs require the gut IEL GLP-1R to selectively restrain local and systemic T cell-induced are mediated by the suppression of gut IEL effector functions linked to the dampening of proximal T cell These data reposition key roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R

September 2022 "The activation of phospholipase C (PLC) is thought to have a key role in the cardiomyocyte response to several different hypertrophic agents such as norepinephrine, angiotensin II and endothelin-1. PLC activity results in the generation of diacylglycerol and inositol trisphosphate, which are downstream signal transducers for the expression of fetal genes, increased protein synthesis, and subsequent cardiomyocyte growth. In this article, we describe the signal transduction elements that regulate PLC gene expression. The discussion is focused on the norepinephrine- α1-adrenoceptor signaling pathway and downstream signaling processes that mediate an upregulation of PLC isozyme gene expression. Evidence is also indicated to demonstrate that PLC activities self-regulate the expression of PLC isozymes with the suggestion that PLC activities may be part of a coordinated signaling process for the perpetuation of cardiac hypertrophy. Accordingly, from the information provided, it is plausible that specific PLC isozymes could be targeted for the mitigation of cardiac hypertrophy." Read more at the source #DrGPCR #GPCR #IndustryNews

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

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling pathway because of its quantifiable stimulus, non-redundancy of genes, and immense importance in vision. We summarize recent discoveries that have advanced our understanding of rod outer segment (ROS) morphology and the pathological basis of retinal diseases. We have combined recently published cryo-electron tomography (cryo-ET) data on the ROS with structural knowledge on individual proteins to define the precise spatial limitations under which phototransduction occurs. Although hypothetical, the reconstruction of the rod phototransduction system highlights the potential roles of phosphodiesterase 6 (PDE6) and guanylate cyclases (GCs) in maintaining the spacing between ROS discs, suggesting a plausible mechanism by which intrinsic optical signals are generated in the retina." Read more at the source #DrGPCR #GPCR #IndustryNews

February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. We explain in detail steps shared between the two sample preparation strategies, including expression and isolation of A2AAR and assembly of A2AAR in lipid nanodiscs and procedures for incorporation of either 19F-NMR or fluorescence probes. Protocols for SMF experiments include sample setup, data acquisition, data processing, and error analysis. For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and Sušac et al. (2018)." Read more at the source #DrGPCR #GPCR #IndustryNews