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Results found for "Stephen S G Ferguson"
- RGS7-ATF3-Tip60 Complex Promotes Hepatic Steatosis and Fibrosis by Directly Inducing TNFα
August 2022 "Aims: The pathophysiological mechanism(s) underlying non-alcoholic fatty liver disease ( Here, we sought to investigate the role of Regulator of G Protein Signaling 7 (RGS7) in hyperlipidemia-dependent
- New role of β-arrestins in MOR signaling
Opioid receptors belong to class A of G protein-coupled receptors or GPCRs and signaled mainly through This report highlights a mechanism of β-arrestin pathway activation dependent on G protein activation Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5391-3. doi: 10.1073/pnas.90.12.5391. Faouzi A, Varga BR, Majumdar S. Biased Opioid Ligands. Shiraki A, Shimizu S.
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the Capturing the dynamics of GPCR activation has always been a challenge because G protein activation in Concurrently, the α1 helix extends, propagating structural changes throughout the G protein. Physiological roles of G protein-coupled receptor kinases and arrestins. Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).
- Why “Displacement” Misleads You: Allosteric Binding Demystified
Kenakin introduces the Hall model : a cube mapping allosteric and orthosteric interactions, layered with G a cooperativity constant : α: Modulator’s effect on radioligand binding σ: Modulator’s effect on G The G Protein Bottleneck: Why Stoichiometry Matters In a standout case study, Kenakin shows how G protein fails to reduce binding of a labeled NAM—not because of irreversibility, but because there isn’t enough G Add G protein. Suddenly, the agonist works .
- 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 However, GRK3’s functions and clinical utility in GAC progression and metastases are unknown.
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
We previously demonstrated that the G protein-coupled receptor (GPCR) arginine vasopressin receptor type1A CRPC cell proliferation through cAMP/protein kinase A signaling, consistent with AVPR2 coupling to the G protein subunit alpha s.
- Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling
G protein-coupled receptors (GPCRs) are integral membrane proteins crucial for sensing extracellular Central to GPCR function are G proteins, comprising subfamilies such as Gs, Gi/o, Gq/11, and G12/13, and a G protein detector tagged with an Nluc donor. Gilman, A.G., G proteins: transducers of receptor-generated signals. Wan, Q., et al., Mini G protein probes for active G protein-coupled receptors (GPCRs) in live cells.
- 📰 GPCR Weekly News, July 1 to 7, 2024
CXV: The Class F of G Protein-Coupled Receptors Yusman Manchanda, Dr. Alejandra Tomas, et al. for their research on Engineered mini-G proteins block the internalization of Jianming Han, Tao Che for their analysis of GPCR-G protein selectivity revealed by structural pharmacology Drs Christopher Langmead, Gregory Stewart, et al. for their study on Molecular insights into orphan G GPCR Activation and Signaling GPCR-MAPK signaling pathways underpin fitness trade-offs in whitefly G
- Harnessing Deep Mutational Scanning for Enhanced Drug Discovery
M., Stephany, J. J., & Fields, S. (2014). G., Coyote-Maestas, W., & Aashish Manglik. (2024). Molecular basis of proton-sensing by G protein-coupled receptors. BioRxiv (Cold Spring Harbor Laboratory) . https://doi.org/10.1101/2024.04.17.590000 Pines, G., Fankhauser G., & Eckert, C. A. (2020). Predicting Drug Resistance Using Deep Mutational Scanning.
- 📰 GPCR Buzz: August 5-11, 2024 | Top Highlights from DrGPCR University!
s Check out the details of each course below: Open to the Public: Enrollment is Now Available! concentrations induces toxicity across multiple generations associated with inhibition in germline G human induced pluripotent stem cell-derived nociceptive-like neurons Methods & Updates in GPCR Research G protein-coupled receptor (GPCR) pharmacogenomics Visualization of endogenous G proteins on endosomes
- Finding needles in haystacks: Omass unveils pipeline aimed at tough-to-drug targets
November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd.’s The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute
- Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024
GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled function of the Adhesion GPCR Latrophilin-1 controls multiple processes in reproduction of C. elegans The G reveals a role for DNAJC13 in DOR downregulation GPCRs in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors in acute kidney injury Ligand-Dependent and G Protein-Dependent Properties Natural Products and Compounds: Potential Therapeutic Targets for the Treatment of Neurological Disease s
- Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin...
Here, we discovered that the epithelial-cell-derived antimicrobial peptides defensins activated orphan G-protein-coupled Defensins and Mrgpra2 were critical for combating S. aureus infections and the formation of neutrophil
- Exploring the Breakthroughs in GPCR Research
Mikel Garcia-Marcos for their work on Get ready to sharpen your tools:A short guide to heterotrimeric G Sokrat, Michel Bouvier, et al. for their study on the Role of the V2R-βarrestin-Gβγ complex in promoting G the chagas disease vector Rhodnius Prolixus (Stål) Role of the V2R-βarrestin-Gβγ complex in promoting G as Potential Drugs for Chronic Myeloid Leukemia Methods & Updates in GPCR Research High-throughput G GPCRs: Insights into Multi-Receptor Pharmacology for the Treatment of Metabolic Disease Relevance of G
- 📰 GPCR Weekly News, February 26 to March 3, 2024
Structure-guided engineering of biased-agonism in the human niacin receptor via single amino acid substitution G Bicarbonate signalling via G protein-coupled receptor regulates ischaemia-reperfusion injury GPCRs in Commentary: Analyzing invertebrate bitopic cadherin G protein-coupled receptors that bind cry toxins of Bacillus thuringiensis Industry News Domain Therapeutics announces the promotion of Stephan Schann and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein
- 📰 GPCR Weekly News, July 31 to August 6, 2023
Randy Hall's study: GPR37L1's role in shaping cortical astrocytes during development Dr. dynamic simulations Kinetic insights into agonist-dependent signalling bias at the pro-inflammatory G-protein Septerna: $150 Million Raised To Discover And Advance Novel Oral Small Molecule Medicines Targeting G Protein-Coupled Receptors Novo Nordisk A/S: Semaglutide 2.4 mg reduces the risk of major adverse cardiovascular
- 📰 GPCR Weekly News, June 17 to 23, 2024
al., for their work on Conformation- and activation-based BRET sensors differentially report on GPCR-G Samuel Liu, Preston Anderson, Sudarshan Rajagopal, Robert Lefkowitz, Howard Rockman for their review G scaffolding proteins required for Shh-mediated axon guidance GPCRs in Oncology and Immunology Regulator of G from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer cells by targeting PAR-1 G protein coupling Reviews, GPCRs, and more Proteome-wide analysis reveals G protein-coupled receptor-like
- 📰 GPCR Weekly News, June 3 to June 9, 2024
Adhesion GPCRs A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets for breast cancer GPCR Activation and Signaling The TAS1R2 G-protein-coupled receptor is an ambient polymerase II degradation Growth factor-dependent phosphorylation of Gαi shapes canonical signaling by G protein-coupled receptors Kinetic Model for the Desensitization of G Protein-Coupled Receptor RNA-seq in mouse mammary epithelial cells GPCR Binders, Drugs, and more Structure-based identification of a G
- Do You Believe AI Could Accelerate Drug Discovery?
G protein-coupled receptors (GPCRs) are major drug targets, yet their complex and dynamic structures This study examines these concerns by comparing AF2's predictions with experimental structures for docking This validates AF2's potential in enhancing drug discovery precision and efficiency.
- 📰 GPCR Weekly News, June 10 to 16, 2024
Gonzalez-Hernandez, Hermany Munguba, Joshua Levitz for their work on Emerging modes of regulation of neuromodulatory G GPCR Activation and Signaling Emerging modes of regulation of neuromodulatory G protein-coupled receptors Astrocytic PAR1 and mGluR2/3 control synaptic glutamate time course at hippocampal CA1 synapses Regulator of G dorsolateral striatum of adult male mice Methods & Updates in GPCR Research RNA therapeutics in targeting G suppress hormones GPCR Events, Meetings, and Webinars June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled domain (WAP) is necessary for this modulatory activity, although data from GST pull-down (glutathione-S-transferase
- Ode to GPCRs
Edwin G. Edwin G. Alfred G. S. of. S. Non-traditional roles of G protein-coupled receptors in basic cell biology.
- 📰 GPCR Weekly News, February 5 to 11, 2024
selectivity of the Ca2+-sensing receptor GPCRs in Cardiology, Endocrinology, and Taste G protein-coupled Doxorubicin alters G-protein coupled receptor-mediated vasocontraction in rat coronary arteries GPCRs development updates Methods & Updates in GPCR Research GPCR-BERT: Interpreting Sequential Design of G Protein-Coupled Receptors Using Protein Language Models Scaling up Functional Analyses of the G Protein-Coupled Extracellular Domain Conformational Changes and Parathyroid Hormone Type 1 Receptor Activation in Class B1 G
- What's Going On with GPCRs?! Find Out in This Week's Update! ⦿ Nov 4 - 10, 2024
Mutational Scanning for Enhanced Drug Discovery Cam Sinh Lu GPCR-BSD: a database of binding sites of human G-protein receptor potential canonical 3 ion channel Smad transcription factors as mediators of 7 transmembrane G protein-coupled receptor signalling The voltage sensitivity of G-protein coupled receptors: Unraveling Affinity of Hemocyte Membrane Preparations of Manduca sexta and Identification of the Receptor-Associated G Structural and Molecular Insights into GPCR Function GPCR-BSD: a database of binding sites of human G-protein
- 📰 GPCR Weekly News, January 1 to 7, 2024
Adhesion GPCRs The adhesion G-protein-coupled receptor mayo/CG11318 controls midgut development in Drosophila development and diseases GPCR Activation and Signaling Proinflammatory chemokine CXCL14 activates MAS-related G regeneration GPCRs in Neuroscience Astrocyte growth is driven by the Tre1/S1pr1 phospholipid-binding G Characterization of the real-time internalization of nine GPCRs reveals distinct dependence on arrestins and G and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein
- Unlocking the Future of Medicine: Advancements in GPCR Research
Trogdon, J Silvio Gutkind, Edward C Stites, et al., for their study on Systems modeling of oncogenic G-protein activation Chiara D Mancinelli, Joshua Levitz, David Eliezer, et al. for their research on Control of G Structural and Molecular Insights into GPCR Function Entropy drives the ligand recognition in G-protein-coupled insights into ligand recognition, selectivity, and activation of bombesin receptor subtype-3 Control of G Pharmaceuticals to Report Second Quarter 2024 Financial Results on August 8, 2024 Dynamic nature of G-protein
- Co-activation of GPCRs facilitate GIRK-dependent current
One potent form of inhibition is mediated by the activation of two inhibitory G protein-coupled receptors Each of these receptors activates G protein-coupled inwardly rectifying potassium (GIRK) channels. The results indicate that a low tonic level of G βγ results in facilitation of GIRK current and a high level of G βγ results in occlusion. in the context of other G protein-coupled receptors."
- 📰 GPCR Weekly News, May 6 to 12, 2024
Sara Marsango and Graeme Milligan for their research on the Regulation of the pro-inflammatory G protein-coupled biological control GPR84 in physiology-Many functions in many tissues Regulation of the pro-inflammatory G regulation of GPR84 in human neutrophils Large-scale deorphanization of Nematostella vectensis neuropeptide G transfer Bayesian network models identify cooperative GPCR:G protein interactions that contribute to G epigenomic signatures Lipid regulation of the glucagon receptor family Technologies for the discovery of G
- AlphaFold’s Breakthrough in GPCR Research: Revolutionizing Discovery, Yet Awaiting Experimental Proof
Before the advent of AlphaFold, homology modeling was the most common method for predicting G protein-coupled While AlphaFold2’s ability to predict static structures was groundbreaking, however, GPCRs are highly
- 📰 GPCR Weekly News, May 27 to June 2, 2024
ligands via nanobody tethering Elk Kossatz, Michel Bouvier, Jana Selent, et al. for their study on G and Signaling Highly biased agonism for GPCR ligands via nanobody tethering Mechanistic insights into G-protein the Metabolite Receptor HCAR3 Regulates Epithelial Proliferation, Migration, and Cellular Respiration G through comprehensive genome sequence analysis in India Methods & Updates in GPCR Research Engineering G proteins: neither single nor simple Structural and Molecular Insights into GPCR Function Insights on the G