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Results found for "GPCR Research"
- GRK3 is a poor prognosticator and serves as a therapeutic target in advanced gastric adenocarcinoma
September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the GPCR-kinase 3 (GRK3) is critical for GPCR signaling. Read more at the source #DrGPCR #GPCR #IndustryNews
- PAR-Induced Harnessing of EZH2 to β-Catenin: Implications for Colorectal Cancer
September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and In addition, the molecular mechanisms underlying GPCR-induced post-translational signaling regulation Read more at the source #DrGPCR #GPCR #IndustryNews
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
Read more at the source #DrGPCR #GPCR #IndustryNews 5-HT2AR, GPCR, hallucinogens, in vitro assay, psychedelics
- Molecular creativity in drug discovery
Innovative Approaches in GPCR Drug Discovery: Designing Precise Solutions for GPCR Challenges. GPCR Podcast: Leadership, Impact, and GPCR Signaling with Dr. GPCR evolved from a grassroots effort to a global force in GPCR science—one rooted in connection, sustainability The pace of GPCR innovation is accelerating. No matter where you are in your GPCR journey, Dr.
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
Read more at the source #DrGPCR #GPCR #IndustryNews
- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival. tumor-adjacent tissues by retrieving TCGA data and detected the expression of GPR39 in colon cancers with qPCR several other biomarkers including PPARG, EPCAM, and PD-L1 was investigated by re-analyzing TCGA data, qPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Molecular targets of psychedelic-induced plasticity
August 2022 "Psychedelic research across different disciplines and biological levels is growing at a Read more at the source #DrGPCR #GPCR #IndustryNews
- PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal...
MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Endogenous ligand recognition and structural transition of a human PTH receptor
Read more at the source #DrGPCR #GPCR #IndustryNews
- Activation of GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through...
Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of...
G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous work directly compares the performance of these novel deep learning-based protein modeling methods for GPCRs We collected the experimentally determined structures of 73 GPCRs from the Protein Data Bank. Read more at the source #DrGPCR #GPCR #IndustryNews
- High GPER expression in triple-negative breast cancer is linked to pro-metastatic pathways and...
September 2022 High GPER expression in triple-negative breast cancer is linked to pro-metastatic pathways According to the cutoff value, 26.4% (95/360) of patients showed high GPER expression and significant In quantitative comparison, GPER abundance is correlated with the high-risk subtype of TNBC. Furthermore, univariate analysis confirmed that GPER was a significant prognostic factor for DMFS in Read more at the source #DrGPCR #GPCR #IndustryNews
- Radioligands vs. Fluorescent Ligands: Binding Assays
Understanding receptor-ligand interaction is key in drug discovery and biomedical research. Radioligands have been used to study GPCRs for decades, but with the advances in the fluorescence field This can be done with agonists, antagonists, reverse agonists in the case of GPCRs. Figure 1. GPCR-radioligand binding assays. Fluorescent ligands: Bringing light to emerging GPCR paradigms.
- Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to...
Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter
- Tracking receptor motions at the plasma membrane reveals distinct effects of ligands on CCR5...
August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational However, how these states impact GPCRs biological function and therapeutic targeting remains incompletely quantitative analysis revealed agonist-like properties of gp120s. " Read more at the source #DrGPCR #GPCR
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future
October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, Read more at the source #DrGPCR #GPCR #IndustryNews
- The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
Read more at the source #DrGPCR #GPCR #IndustryNews
- GBCRdb for beginners
Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates axonal...
G protein-coupled receptor 3 (GPR3) belongs to the class A rhodopsin-type GPCR family and is highly expressed Read more at the source #DrGPCR #GPCR #IndustryNews
- Combined docking and machine learning identify key molecular determinants of ligand pharmacological
September 2022 "G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases A central question of GPCR drug discovery is to understand what determines the agonism or antagonism ligands made interactions with W2866.48×48 and Y3167.43×42, both residues considered to be important in GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though Read more at the source #DrGPCR #GPCR #IndustryNews
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
Although some GPCRs constitutively internalize through clathrin-coated pits independently of phosphorylation In this study, it is revealed that CCR2 scavenging role was largely independent of the classical GPCR Check the original article at https://pubmed.ncbi.nlm.nih.gov/36719944/ #GPCR #DrGPCR#Ecosystem
- G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease..
October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling signaling produce discrete and separable effects and provide proof of concept for the development of safer GPCR-targeting Read more at the source #DrGPCR #GPCR #IndustryNews
- GPR108 is required for gambogic acid inhibiting NF-κB signaling in cancer
September 2022 "GPCRs are the most potential targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer drug is not fully investigated. Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews
- GPCR voltage dependence controls neuronal plasticity and behavior
G-protein coupled receptors (GPCRs) play a paramount role in diverse brain functions. Almost 20 years ago, GPCR activity was shown to be regulated by membrane potential in vitro, but whether the voltage dependence of GPCRs contributes to neuronal coding and behavioral output under physiological Here we show that muscarinic GPCR mediated neuronal potentiation in vivo is voltage dependent. crucial involvement of GPCR voltage dependence in neuronal plasticity and behavior.
- Odorant receptors – a bit of smell for drug discovery
function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR OR51E1 and OR51E2, initially assumed to be GPCRs only expressed in prostate tissue, play a role in prostate compounds, there has been a growing interest from the scientific community to target this class of GPCRs Future directions Important directions in ORs research to advance drug discovery include the deorphanization Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem
- Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic di
AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Read more at the source #DrGPCR #GPCR #IndustryNews
- Label-free LC-MS based assay to characterize small molecule compound binding to cells
In one example, to study a G protein coupled receptor (GPCR), we used one antagonist as probe and multiple Read more at the source #DrGPCR #GPCR #IndustryNews
- The regulation of PKA signaling in obesity and in the maintenance of metabolic health
of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- N-Acyl Amides from Neisseria meningitidis and Their Role in Sphingosine Receptor Signaling
30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews



