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- Adenosine receptor signalling in Alzheimer's disease
Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- 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
- Pharmacologic Models
GPCR News. Elevate your pharmacology expertise. Unlock "Pharmacologic Models" now
- 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
- N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 ...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR libraries have complementary advantages and illustrate how access to high-resolution structures of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Molecular insights into psychedelic drug action
Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
Read more at the source #DrGPCR #GPCR #IndustryNews
- Molecular creativity in drug discovery
In this new course, Dr. Terry Kenakin reveals how drug chemistry defines function, not just fit. GPCR Podcast: Leadership, Impact, and GPCR Signaling with Dr. with real-world acceleration, strategic consulting, and CRO matchmaking. • Premium Expansion : New courses on-demand expert frameworks, and member-only discounts. 🔹 Who is it for? Access this week’s full Premium Edition here ➤ Voice of the Community “Thank you for bringing this course
- Dr. GPCR Virtual Cafe with Matthew Eddy - New date!
GPCR Virtual Cafe session with Dr. Matthew E. on Friday, October 7th at 1 PM ET.
- Novel Driver Strength Index highlights important cancer genes in TCGA PanCanAtlas patients
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
- 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...
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
- 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
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
- A broad look into the future of systemic sclerosis
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
- 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
- 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
