Previous findings suggest that parallel pathways independently relay innate threat signals from different Yet little is known about whether and how multi-sensory innate threat cues are integrated and conveyed The identification of unified innate threat pathways may provide insights into developing therapeutic candidates for innate fear-related disorders."

In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types. study, for the first time, we demonstrate the nuclear localization of H2R in lymphatic endothelial cells

October 2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of -2 receptor (GLP-2R) antagonists are needed. Experimental approach: COS-7 cells were transfected with the human GLP-2R and assessed for cAMP accumulation or competition binding using 125 I-GLP-2(1-33)[M10Y]. To examine selectivity, COS-7 cells expressing human GLP-1 or GIP receptors were assessed for cAMP accumulation

September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell carcinoma: an emerging prognostic indicator and future therapeutic target " Purpose: Beta 2-Adrenergic significance in relation with the clinicopathological features and overall survival of oral squamous cell analyze β2-AR protein and mRNA levels in a total of 65 histopathologically confirmed OSCC tissues (case group ) and 65 normal tissues (control group) from the oral cavity."

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that

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 the VFT domains and/or HH bundle intraloop-2 or intraloop-3.

October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable,

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative 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

functions through the activation of the G protein-coupled receptors (GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations in the PK2 and PKR2 genes are involved in the pathogenesis of KS. of PK2/PKR2 activity by anosmin 1, since this protein is able to enhance the activation of the ERK1/2 (extracellular signal-regulated kinase 1/2) pathway elicited by PK2 through PKR2.

September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system

Screening Reveals that the Metabolite Receptor HCAR3 Regulates Epithelial Proliferation, Migration, and Cellular regulates the expression and alternative splicing of genes associated with aphasia-related diseases in PC12 cells inverse agonist improves lung functioning in preclinical asthma GPCR Events, Meetings, and Webinars June 2 Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2 Scientist Senior Research Associate/Associate Scientist, Protein Science Post-Doctoral Fellow—Pharmacology/Cell

Here, we discovered that the epithelial-cell-derived antimicrobial peptides defensins activated orphan

Save the dates: November 2 - 4: We're sponsoring the GPCR Retreat and would love to meet you there! GPCR Events, Meetings, and Webinars October 25 - 27, 2023 | 3rd Annual Meeting IRN I-GPCRNet November 2 May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2

July 2022 " G.CLIPS biotech is 2 years old today🎂.

Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β -Arrestin Interaction The β 2-adrenergic receptor ( β 2AR) is a prototypical and extensively studied GPCR that can provide This single point mutation in extracellular loop 2 of the β 2AR is sufficient to intrinsically bias the the extracellular loops of the receptor and the extracellular pocket formed by transmembrane domains 2, Our studies reveal that F193 in extracellular loop 2 in the β2-adrenergic receptor mediates interactions

and Immunology Dynamic Phosphoproteomics of BRS3 Activation Reveals the Hippo Signaling Pathway for Cell expression of GPR50 promotes the proliferation, migration and autophagy of hepatocellular carcinoma cells Gi/o GPCRs drive the formation of actin-rich tunneling nanotubes in cancer cells via a Gβγ/PKCα/FARP1 Comparative analysis of the occupancy of Histone H3 Lysine 4 methylation in the cells treated with TGFβ Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells.

., for their study on Cell swelling enhances ligand-driven β-adrenergic signaling ✨ Reserve Your seat This technique for studying cell receptors could have sweeping implications for drug development DeepCure team is excited to welcome Justin Potnick, to our Medicinal Chemistry group Call for GPCR Papers Emerging , 2024 | 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based plate homeostasis through IHH Signaling GPCR Activation and Signaling Illuminating GPCR trafficking Cell

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 cell proliferation by enhancing the ERK pathway. Methods & Updates in GPCR Research Small Molecule Tools to Study Cellular Target Engagement for the Intracellular July 2 - 7.

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 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells "β-arrestins mediate regulatory processes for over 800 different G However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. Employing GRK knockout cells and β-arrestins lacking the finger-loop-region, we show that the two isoforms advanced NanoLuc/FlAsH-based biosensors reveals distinct conformational signatures of β-arrestin1 and 2

September 2022 Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal transduce signals across the plasma membrane and orchestrate a multitude of physiological processes within cells residue in a cholesterol recognition/interaction amino acid consensus (CRAC) motif in transmembrane helix 2

September 2022 Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of

April 2022 Addex Therapeutics Completes Patient Enrollment For Dipraglurant Blepharospasm Phase 2 Clinical

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause

August 2022 Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in psychiatric and neurological conditions, today announced positive topline results from its Phase 3 EMERGENT-2 statistically significant reduction of symptoms, as assessed by PANSS total score, starting at Week 2

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron However, intracellular partners linking GPCRs to TASK1 modulation are not yet well-known. We hypothesized that isoform 2 of rho-kinase (ROCK2), acting as downstream GPCRs, mediates adjustment

It is classified into two types: Sigma-1 (S1R) and Sigma-2 (S2R) based on their biological functions. We have explored hydrophobic groups of different sizes on both sides of the five-membered ring scaffold