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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 What are the implications in drug discovery? Check the original article at https://pubmed.ncbi.nlm.nih.gov/36719944/ #GPCR #DrGPCR#Ecosystem

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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 "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

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

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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

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 better tools to study its function in both disease and physiological settings will likely potentiate drug discovery campaigns against this orphan GPCR. #GPCR #DrGPCR#Ecosystem

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However, these drugs show adverse effects, including increased blood pressure in mirabegron patients. Hence, new β3 -AR agonists are needed as starting points for drug development. Read more at the source #DrGPCR #GPCR #IndustryNews

Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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

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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

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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

Sulfo-glyco barcode - perspectives and added value in drug discovery A growing body of evidence proposes It remains to be discovered how much the modulation of these PTMs is relevant for future drug design. There are few examples of the applicability of the sulfo-glyco barcode in drug discovery. Check the original article at https://pubmed.ncbi.nlm.nih.gov/36729338/ #GPCR #DrGPCR#Ecosystem

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

October 2022 Design and validation of recombinant protein standards for quantitative Western blot analysis 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 This renders full-length recombinant GPCRs useless for analytical purposes, a problem that can be overcome Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery platform technology platform, which uses conformationally selective VHH antibodies – ConfoBodies® – to stabilize GPCRs conformations, will be applied with the goal of enabling the discovery of novel therapeutic antibody drug candidates. " Read more at the source #DrGPCR #GPCR #IndustryNews

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

of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

showed that the receptor is a member of the Octβ3 protein family, and an analysis using quantitative PCR pharmacological properties and functions of PxOctβ3 in P. xylostella, thus, providing a theoretical basis for the design Read more at the source #DrGPCR #GPCR #IndustryNews

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Methods: Immunohistochemistry, western blot and quantitative real-time PCR techniques were used to analyze Read more at the source #DrGPCR #GPCR #IndustryNews