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Results found for "GPCR webinar series"
- 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
- 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
- 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
- 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
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
crystal structure of the human S1P5 receptor in complex with a selective inverse agonist determined by serial Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- 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
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
GPCR Weekly News Free Edition—your clear, credible signal in a noisy field. GPCR Forum to Biophysics; plus targeted summits for discovery teams planning 2025–2026. GPCR members save 50%+ (check your Weekly News code). Speed: faster GPCR target validation and assay development. The pace of GPCR innovation is accelerating.
- N-Acyl Amides from Neisseria meningitidis and Their Role in Sphingosine Receptor Signaling
obligate human pathogen N. meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR) S1PR4. Read more at the source #DrGPCR #GPCR #IndustryNews
- Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR
- Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone...
glucose-dependent insulinotropic polypeptide (GIP) which exert their functions through G protein-coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- 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. Read more at the source #DrGPCR #GPCR #IndustryNews
- Pharmacological Properties and Function of PxOctβ3 Octopamine Receptor in Plutella xylostella (L.)
A series of octopamine receptor agonists and antagonists were tested against PxOctβ3. showed that the receptor is a member of the Octβ3 protein family, and an analysis using quantitative PCR Read more at the source #DrGPCR #GPCR #IndustryNews
- 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. that would allow for lower dose utilization of opioid analgesics. " Read more at the source #DrGPCR #GPCR
- Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell...
Methods: Immunohistochemistry, western blot and quantitative real-time PCR techniques were used to analyze Read more at the source #DrGPCR #GPCR #IndustryNews
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- All About Addgene: More Open and Reproducible Science with Materials Sharing
GPCR Virtual Cafe? Register today! Addgene's Dr. Joanne Kamens is our guest. research or you want to share your materials, this is the place to go. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe / #gpcr #drgpcr #virtualcafe #addgene
- Enhanced membrane binding of oncogenic G protein αqQ209L confers resistance to inhibitor YM-254890
October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular They can also function independently of GPCR activation upon acquiring mutations that prevent GTPase YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L GPCR-dependent signaling by PM-restricted wild type αq is strongly inhibited by YM, demonstrating that Read more at the source #DrGPCR #GPCR #IndustryNews
- Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response
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. Figure 2.Assay Principle: TR-FRET assay using CELT-335, a dual (CB1/CB2) fluorescent ligand that serves for CB1R in live cells and the PHERAstar FSX is the ideal microplate reader for characterizing the GPCR-ligand
- Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but...
Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor (GPCR 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
- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of...
Protein in the Allosteric Regulation of Adhesion Receptor GPR97 "Adhesion G-protein-coupled receptors (aGPCRs )-a major family of GPCRs-play critical roles in the regulation of tissue development and cancer progression The orphan receptor GPR97, activated by glucocorticoid stress hormones, is a prototypical aGPCR. of the Go protein, and offers guidance for future drug design of aGPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews
- Therapeutic validation of an orphan G protein‐coupled receptor
Historically, ligands for GPCRs have been identified before their receptor counterparts. Therefore, matching a ligand to an orphan GPCRs, the process of de-orphanizing, is of great importance GPR84 antagonists include a series of dihydropyrimidinoisoquinolinones (Labéguère et al., 2014), which From these series of compounds, GLPG1205 progressed into clinical development for the potential treatment #GPCR #DrGPCR#Ecosystem
- Endocannabinoid System in the Neuroendocrine Response to Lipopolysaccharide-induced Immune Challenge
Read more at the source #DrGPCR #GPCR #IndustryNews
- Neuropeptide S Encodes Stimulus Salience in the Paraventricular Thalamus
Read more at the source #DrGPCR #GPCR #IndustryNews
