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Results found for "GPCR Pharmacology"
- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
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- Endosomal parathyroid hormone receptor signaling
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
- AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide Extensive efforts of structural biology have been made on the study of GPCRs. However, a large portion of GPCR structures remain unsolved due to structural instability. Herein we evaluated the accuracy of GPCR structure models predicted by AlphaFold2. Read more at the source #DrGPCR #GPCR #IndustryNews
- The microglial endocannabinoid system similarly regulated by lipopolysaccharide and interferon gamma
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- Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of...
September 2022 Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of immunotherapy in triple-negative breast cancer "Quantitative systems pharmacology (QSP) modeling is Read more at the source #DrGPCR #GPCR #IndustryNews
- GB83, an Agonist of PAR2 with a Unique Mechanism of Action Distinct from Trypsin and PAR2-AP
October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by bona fide agonist of PAR2 that uniquely modulates PAR2-mediated cellular signaling and is a useful pharmacological Read more at the source #DrGPCR #GPCR #IndustryNews
- Novel Driver Strength Index highlights important cancer genes in TCGA PanCanAtlas patients
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- Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and...
October 2022 Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717, and a G protein-coupled receptor (GPCR)-based antagonist that blocks the profibrotic activity of endothelial Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and Read more at the source #DrGPCR #GPCR #IndustryNews
- Molecular creativity in drug discovery
Welcome GPCR Fans, Most pharmacologists are trained to chase targets. Upcoming events: Global GPCR summits and pharmacology forums shaping 2026 priorities. GPCR Podcast: Leadership, Impact, and GPCR Signaling with Dr. scientists. 👉 Dive into spatial pharmacology ➤ A Note From Yamina: Building the Next Chapter of Dr. GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who
- A broad look into the future of systemic sclerosis
Pharmacological interventions, although for other indications, are already in clinical use to address Read more at the source #DrGPCR #GPCR #IndustryNews
- Endogenous ligand recognition and structural transition of a human PTH receptor
light on the distinct durations of signaling induced by PTH and PTHrP" Read more at the source #DrGPCR #GPCR
- GRK3 is a poor prognosticator and serves as a therapeutic target in advanced gastric adenocarcinoma
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. Through genetic and pharmacologic modulations of GRK3, a series of functional and molecular studies were Read more at the source #DrGPCR #GPCR #IndustryNews
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
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 Read more at the source #DrGPCR #GPCR #IndustryNews
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
perception, and thought, and have the activation of serotonin (5-HT) 2A receptors (5-HT2A Rs) as a main pharmacological Read more at the source #DrGPCR #GPCR #IndustryNews 5-HT2AR, GPCR, hallucinogens, in vitro assay, psychedelics
- 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
- GPCR Updates: Celebrating Breakthroughs, New Course Launches Soon, and Exclusive Discounts! | Aug 26 - Sep 1, 2024
upcoming events, and our newly announced pharmacology courses. pharmacologic activity measurement, mechanisms of action, and GPCR discovery strategies. Secure your spot today and elevate your pharmacology expertise! Papers Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs HIGHLIGHT Research Associate
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
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- Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface
Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia caused...
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
- PAR-Induced Harnessing of EZH2 to β-Catenin: Implications for Colorectal Cancer
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
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
Temperature optimization and application to cell-based kinetic studies "G protein-coupled receptors (GPCRs The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. for drug discovery" Read more at the source #DrGPCR #GPCR #IndustryNews
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
Read more at the source #DrGPCR #GPCR #IndustryNews
- The expression and clinical significance of GPR39 in colon cancer
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
- PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal...
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
- Endogenous ligand recognition and structural transition of a human PTH receptor
Read more at the source #DrGPCR #GPCR #IndustryNews
- Activation of GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through...
Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of...
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
- 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, development and progress in optimising physicochemical properties, understanding advanced molecular pharmacology 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
- 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 development and progress in optimizing physicochemical properties, understanding advanced molecular pharmacology Read more at the source #DrGPCR #GPCR #IndustryNews


