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- Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water ...
Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early evolution of eukaryotic species, therefore, the genome-wide identification of GPCR genes can provide Here, we identified a total 216 full-length GPCR genes in the marine water flea Diaphanosoma celebensis In this study, these results may provide a better understanding on the evolution of GPCRs, and expand
- GPCR News Flash! Top Updates You Can't-Miss! + University CheatSheet is finally available! ❄ Dec 2 - 8, 2024
Hello, hello GPCR Buddies! It's starting to look a lot like Christmas at Dr. GPCR! 🎉 Conformational coupling between extracellular and transmembrane domains modulates holo-adhesion GPCR Don't get left in the dust—upgrade now and keep your GPCR gossip game strong! Classified GPCR News Let’s dive into the Classified GPCR News from December 2nd to 8th, 2024 Industry function GPCR Activation and Signaling P2X7R-primed keratinocytes are susceptible to apoptosis via GPCR-Gβγ-pERK
- 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...
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- 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
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- 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
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
GPCR Weekly News Free Edition—your clear, credible signal in a noisy field. GPCR members save 50%+ (check your Weekly News code). Speed: faster GPCR target validation and assay development. The pace of GPCR innovation is accelerating. I couldn’t be happier you created this podcast." — DrGPCR Podcast Listener Upgrade to Premium and turn
- The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
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
- 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
- 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
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
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- 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
- 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. 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
