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Results found for "GPCR data platform"
- 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
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
Temperature optimization and application to cell-based kinetic studies "G protein-coupled receptors (GPCRs The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. for drug discovery" Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly Buzz: Exciting Schedule Shifts for Principles of Pharmacology I & II | August 12-18, 2024
miss out on insightful resources like ' Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR Pharmacology .' GPCR Event Spotlight 11th Adhesion GPCR Workshop Location: Mexico City Dates: October 23-25, Let’s dive into the Classified GPCR News from August 12th to 18th, 2024 Adhesion GPCRs Heterogeneity screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November
- Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
Finally, inhibition of Gq-GPCR coupling in mice enhanced the antinociceptive effects of morphine. These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation that would allow for lower dose utilization of opioid analgesics. " Read more at the source #DrGPCR #GPCR
- A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New..
Transcript and protein levels were determined by RT-qPCR and Western blot, respectively. These data suggest that hypoxia-dependent activation of A2B adenosine receptor promotes survival of GSCs 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
- GPCRS: AN ODYSSEY FROM STRUCTURE, SIGNALING AND REGULATION TO THERAPEUTICS
meeting is to bring together a highly interdisciplinary group of scientists to exchange new experimental data Spatial-temporal signaling of GPCRs and physiological functions; 2. GPCRs as environmental sensors; 3. New approaches to GPCR drug discovery. This timely meeting will not only provide an inclusive forum for communication, but also a platform for
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
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
- 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
- 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
- Molecular targets of psychedelic-induced plasticity
Read more at the source #DrGPCR #GPCR #IndustryNews
- Orion Shares New Data on its Latest Best-in-Class Drug Candidate
), today announced that it will be presenting important new data at both LSX World Congress and TIDES His presentations will describe Orion’s drug discovery platform, one of the fastest drug discovery solutions in the industry for targeting peptidergic GPCRs. Hartley will also present new data on Orion’s CCR2 antagonist, OB-004, demonstrating the ability of this powerful platform to rapidly identify best-in-class GPCR drug candidates."
- GBCRdb for beginners
Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
Read more at the source #DrGPCR #GPCR #IndustryNews
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
GPCR members save 50%+ (check your Weekly News code). 👉 Explore Trailers & Join Today Inside Revvity's R&D: How pHSense Was Born The day your data surprises They translated a fundamental principle of chemistry into a usable platform for pharmacology—showing Cleaner data: higher signal-to-noise ratios sharpen CNS assays. The pace of GPCR innovation is accelerating.
- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
Together, these data reveal a shear-dependent signaling axis of PTK2, integrin αIIbβ3, and CIB1 in collagen Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- 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 In the nervous system, although there is limited data, it has been suggested that ORs adopt functions compounds, there has been a growing interest from the scientific community to target this class of GPCRs Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem
- GPCR Updates: Celebrating Breakthroughs, New Course Launches Soon, and Exclusive Discounts! | Aug 26 - Sep 1, 2024
Hello GPCR Community, Stay up-to-date with the latest GPCR research, including breakthrough studies, protein-coupled receptor structural landscape: Major milestones and future directions . 🎉 New Course Dates GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Classified GPCR News Let’s dive into the Classified GPCR News from August 26th to September 1st, 2024 Papers Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings
- Radioligands vs. Fluorescent Ligands: Binding Assays
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. If you are curious about fluorescent probes, fluorescent probe design or GPCR tools, feel free to contact GPCR-radioligand binding assays. Fluorescent ligands: Bringing light to emerging GPCR paradigms.
- 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
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
Introduction Cannabinoid receptors are GPCRs, and two main types exist, CB1R and CB2R. The data obtained is comparable to those reported in radioligand binding assays (Table 1). Radioligand binding data are from [2,3]. for CB1R in live cells and the PHERAstar FSX is the ideal microplate reader for characterizing the GPCR-ligand
- 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
- 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






