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capacity of microglia to synthesize, degrade, and respond to cannabinoids which has implications for the development Read more at the source #DrGPCR #GPCR #IndustryNews

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GPCR Virtual Cafe session with Dr. Matthew E. on Friday, October 7th at 1 PM ET.

Quantitative real-time probe-based polymerase chain reaction (qRT-PCR) assays are deployed in order to This can be deduced from the qRT-PCR assays; triggering CB1 receptors amplifies both NR4A1 and NR4A3 Read more at the source #DrGPCR #GPCR #IndustryNews

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Hence, new β3 -AR agonists are needed as starting points for drug development. To confirm the activity of the virtual hits, an in vitro assay was conducted, measuring cAMP levels at Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation In this model, GPCR signaling is turned-off by receptor phosphorylation via GPCR kinases (GRKs) and subsequent However, over the last decade, this model has been extended by discovering that some internalized GPCRs Accumulative evidence shows that the location of signaling has an impact on the physiological effects of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

Confers Cholesterol-Induced Thermal Stability to the Serotonin 1A Receptor "G protein-coupled receptors (GPCRs The serotonin1A receptor is a crucial neurotransmitter receptor in the GPCR family involved in a multitude envision that our results could have potential implications in structural biological advancements of GPCRs and design of thermally stabilized receptors for drug development." Read more at the source #DrGPCR #GPCR #IndustryNews

and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor (GPCR Additionally, we employed optical assays in living cells to thoroughly profile both GPR35 isoforms for Read more at the source #DrGPCR #GPCR #IndustryNews

describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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Fibroblasts from SSc patients exhibit a specific signalling and reactivate developmental pathways and Read more at the source #DrGPCR #GPCR #IndustryNews

Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR ) drug development by displaying subtype selectivity and more specific receptor modulation. Read more at the source #DrGPCR #GPCR #IndustryNews

light on the distinct durations of signaling induced by PTH and PTHrP" Read more at the source #DrGPCR #GPCR

signaling potencies for such ligands when assessed on rodent vs human PTH1Rs, as shown by cell-based assays Read more at the source #DrGPCR #GPCR #IndustryNews

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

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by Read more at the source #DrGPCR #GPCR #IndustryNews

) GPR183 in the development of neuropathic pain. Further investigation of the signaling pathways downstream of GPR183 is needed to support the development intrathecal injection of its ligand, 7α,25-dihydroxycholesterol (7α,25-OHC), causes time-dependent development In support, we found that the development of 7α,25-OHC/GPR183-induced mechano-allodynia was associated Read more at the source #DrGPCR #GPCR #IndustryNews

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membranes: an alternative to radioligand binding methods "Background: Replacement of radioligand binding assays antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR GPCRs in general and cannabinoid CB1 receptor in particular show a progressive tendency to aggregate same order of magnitude but slightly higher than values obtained by the radioligand saturation binding assay Read more at the source #DrGPCR #GPCR #IndustryNews

hypercalcemia caused by biased allosteric CaSR autoantibodies "Biased agonism is a frontier field in GPCR insights into the phenotype and characteristics of AHH and the mechanisms by which the biased agonism of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

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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

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

regulating proliferation, inflammation, adhesion, migration, insulin release, muscle relaxation, and cancer development Read more at the source #DrGPCR #GPCR #IndustryNews