Search Results
Results found for "Druggable GPCR"
- A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in...
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
- G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...
representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- GPR110, a receptor for synaptamide, expressed in osteoclasts negatively regulates osteoclastogenesis
Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, GPR110 belongs to adhesion GPCR and was the functional receptor of N-docosahexaenoyl ethanolamine (also Read more at the source #DrGPCR #GPCR #IndustryNews
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR A growing number of GPCRs have been shown to be localized in the nucleus and contribute toward transcriptional At the same time, H2R as a GPCR imparts many unresolved questions, such as the functional relevance of 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
- 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
- Structures of β 1-adrenergic receptor in complex with Gs and ligands of different efficacies
August 2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies Previous studies revealed how ligands with different efficacies activate GPCRs. Here, we investigate how a GPCR activates G-proteins upon binding ligands with different efficacies. These data provide insights into the ligand efficacy in the activation of GPCRs and G-proteins." Read more at the source #DrGPCR #GPCR #IndustryNews
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly The fusion strategies explored here are likely applicable to cryo-EM interrogation of other GPCRs and Read more at the source #DrGPCR #GPCR #IndustryNews
- GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting
pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination analysis of subcellular fractions revealed a cytosolic localization. " Read more at the source #DrGPCR #GPCR
- 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
- 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
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends participate in a molecular mechanism to trigger β-arrestin recruitment. " Read more at the source #DrGPCR #GPCR
- Chemical signaling regulates axon regeneration via the GPCR-Gqα pathway in Caenorhabditis elegans
demonstrate that the chemoreceptor genes, srg-36 and srg-37, which encode G protein-coupled receptors (GPCRs Here, we show that SRG-36 and SRG-37 act as upstream GPCRs that activate EGL-30. SRG-36 and SRG-37 are GPCRs for the dauer-inducing ascaroside, ascr#5. Thus, ascaroside signaling promotes axon regeneration by activating the GPCR-Gqα pathway.
- 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
- Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Inflammation..
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
- Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent ROCK...
In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Read more at the source #DrGPCR #GPCR #IndustryNews
- Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs)...
Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling Read more at the source #DrGPCR #GPCR #IndustryNews
- Pharmacological Properties and Function of PxOctβ3 Octopamine Receptor in Plutella xylostella (L.)
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
- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Novel Driver Strength Index highlights important cancer genes in TCGA PanCanAtlas patients
Read more at the source #DrGPCR #GPCR #IndustryNews
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
Read more at the source #DrGPCR #GPCR #IndustryNews
- Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify...
and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation
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
- 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
- A broad look into the future of systemic sclerosis
Read more at the source #DrGPCR #GPCR #IndustryNews