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- GPCRS: AN ODYSSEY FROM STRUCTURE, SIGNALING AND REGULATION TO THERAPEUTICS
09, 2022 | | SNOWBIRD RESORT, UTAH, UNITED STATES The superfamily of G protein-coupled receptors (GPCRs mechanisms of GPCR function has revealed new paradigms with increasingly complex models of receptor Spatial-temporal signaling of GPCRs and physiological functions; 2. GPCRs as environmental sensors; 3. New approaches to GPCR drug discovery.
- Molecular insights into psychedelic drug action
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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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- 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
- VAMP2: a crucial player in the delivery of MOR to the synapse
Transporting Protein-coupled receptors (GPCRs) to the synapse, where they are involved in neurotransmission From a general overview, after GPCRs synthesis in the endoplasmic reticulum, GPCRs are transported to In the context of GPCR recycling, this process is complex and highly regulated that involves multiple However, the selectivity of SNARE complex proteins to regulate the release of different types of GPCRs /vesicle-associated-membrane-protein-2-is-a-cargo-selective-v-snare-for-a-subset-of-gpcrs #GPCR #DrGPCR
- Novel Driver Strength Index highlights important cancer genes in TCGA PanCanAtlas patients
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- 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
- A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in...
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- 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
- 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 Read more at the source #DrGPCR #GPCR #IndustryNews
- Radioligands vs. Fluorescent Ligands: Binding Assays
Radioligands have been used to study GPCRs for decades, but with the advances in the fluorescence field This can be done with agonists, antagonists, reverse agonists in the case of GPCRs. Figure 1. If you are curious about fluorescent probes, fluorescent probe design or GPCR tools, feel free to contact GPCR-radioligand binding assays. Fluorescent ligands: Bringing light to emerging GPCR paradigms.
- GBCRdb for beginners
Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- 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
- 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. 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
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
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- 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
- A broad look into the future of systemic sclerosis
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- Join Us Today!
GPCR Ecosystem is under construction and dozens of your colleagues are enjoying its benefits! Catch up with the latest #GPCR news, start a discussion in the forum, and much more today! Join the #GPCR movement by becoming a site member for FREE! ➡️ https://www.ecosystem.drgpcr.com/ #gpcr #drgpcr
- 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
- 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
- Endogenous ligand recognition and structural transition of a human PTH receptor
Read more at the source #DrGPCR #GPCR #IndustryNews
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
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
- 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
- 📢 GPCR Update: August 19-25, 2024 | Thrilling Announcement: New Pharmacology Course Dates & Exclusive Discounts Inside!
Topics cover new cellular assays, real-time kinetics, and unique GPCR behaviors. GPCR Event Spotlight 11th Adhesion GPCR Workshop Location: Mexico City Dates: October 23-25, 2024 Connect with peers and delve into cutting-edge adhesion GPCR biology. Let’s dive into the Classified GPCR News from August 19th to 25th, 2024 GPCR Activation and Signaling Papers NEW Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events,




