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Results found for "positive allosteric modulators"

  • 📰 GPCR Weekly News, November 20 to 26, 2023

    Domain Unfolding in Adhesion GPCRs Molecular Sensing in Adhesion GPCR Dissociation Physiological Force Modulation and interface interactions Experimental modulation of physiological force application on leg joint neurons Clinical Pharmacology 2026 GPCR Jobs - Contact Mark Schmeizl NEW Scientist NEW Lead Researcher NEW Post-Doctoral Fellow Sr Scientist in Obesity, Muscle, and Metabolism Post-Doctoral Fellow Research Associate I, Tissue Culture Post-Doc Research Associate Postdoctoral Fellow Explore Dr.

  • From Technician to Trailblazer: How Sokhom Pin Designed His Own PhD Program While Working in Industry

    With a growing family and a full-time position, traditional PhD training just wasn’t an option. A Model for Future Scientists? His hybrid path is a model of possibility for professionals in the biotech industry who still dream of

  • Inside Out: Mapping GPCRs from Membrane Codes to Market Moves

    Additionally, new studies reveal how phosphorylation barcodes shape arrestin engagement, a biased NTSR1 modulator Terry Kenakin, these five modules reveal how location bias, intracellular signaling, and ligand kinetics GRK-Specific Phosphorylation Barcodes Shape Arrestin Engagement with ACKR3   A β-Arrestin-2-Biased NTSR1 Modulator

  • Glyco-sulfo hotspots in the chemokine receptor system

    modifications (PTMs), contribute to the high affinity binding to the positively charged groove on the chemokines through the charge interactions between the negative sulfate groups in the N-terminus and the positively Probing the modulation of O-glycosylation and tyrosine sulfation on CCR5 and CCR1 function In this study mutagenesis approaches were performed to evaluate the effects of O-glycosylation and tyrosine sulfation modulation It remains to be discovered how much the modulation of these PTMs is relevant for future drug design.

  • Unveiling GPCR Priming: The Hidden Synergy in Cellular Signalling

    This unproductive coupling revealed that non-cognate G protein interactions could modulate GPCR signalling In 2017, Gupte et al. introduced GPCR priming, which posits that non-cognate G proteins can enhance the Gupte et al. utilized a systematic protein affinity strength modulation (SPASM) technique to show that development, as targeting these non-cognate interactions could lead to novel therapeutic strategies for modulating

  • Community guidelines for GPCR ligand bias: IUPHAR review 32

    August 2022 "GPCRs modulate a plethora of physiological processes and mediate the effects of one-third implementation of the guidelines, together improving translation from in vitro to disease-relevant in vivo models

  • Regulators of G-protein signaling: essential players in GPCR signaling

    are selective for certain GPCRs, as a proof RGS4 which is expressed in the brain, has been shown to modulate RGS4 is expressed in various immune cells, including T cells and B cells, and has been shown to modulate In conclusion, RGS proteins are essential modulators for the GPCR signaling mediated by G proteins, which Hepler, Cellular regulation of RGS proteins: modulators and integrators of G protein signaling. Traynor, Differential modulation of mu- and delta-opioid receptor agonists by endogenous RGS4 protein

  • Identification of hub genes in the subacute spinal cord injury in rats

    The models of the three gene expression profiles were all for SCI to the thoracic segment of the rat. Module analysis was performed using Cytoscape.

  • Enhancing GPCR Research Outreach | Dr GPCR University early-bird registration ends soon!

    II Peptide Analogues: A Proposed Key Role of the N-Terminal Region for Novel Urotensin II Receptor Modulators Congress of Basic and Clinical Pharmacology GPCR Jobs NEW Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Senior or Lead Researcher   Senior Scientist, Cryo-Electron Microscopy

  • 📰 GPCR Weekly News, January 15 to 21, 2024

    Graham Ladds’ team refines AlphaFold models using binding calculations for human adenosine A3 receptor islets regulating somatostatin release and islet development GPCR Activation and Signaling In Vitro Module activation and signaling GPCR Binders, Drugs, and more Computational Workflow for Refining AlphaFold Models Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs NEW Post-Doc position NEW Lead Researcher Senior Researcher in Structural Biology Post-Doctoral Fellow Postdoctoral

  • G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease..

    Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation Here, we generated a G protein-biased GPR3 mouse model to investigate the physiological and pathophysiological leads to a decrease in the area and compaction of amyloid plaques in the preclinical AppNL-G-F AD mouse model

  • The regulation of PKA signaling in obesity and in the maintenance of metabolic health

    hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR) to modulate Mouse models have provided invaluable information on the roles for PKA subunits in brain and key metabolic

  • 📰 GPCR Weekly News, February 6 to 12, 2023

    Isoform- and ligand-specific modulation of the adhesion GPCR ADGRL3/Latrophilin3 by a synthetic binder Binders, Drugs, and more An antibody-drug conjugate targeting GPR56 demonstrates efficacy in preclinical models Quantitative analysis of sterol-modulated monomer-dimer equilibrium of the β1-adrenergic receptor by pulls off rare IPO, raising $161M 3-drug combo leads to 'unprecedented' response in pancreatic cancer models Protein Biochemistry) Speculative Applications (Mass Spectrometry) Speculative Applications (Chemistry) Post-Doctoral

  • CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via...

    This study aimed to investigate the specific molecular mechanism by which CCR9/CCL25 modulates malignant The effect of CCL25 on the development of SACC in vivo was examined by a xenograft tumor model in nude

  • Unlocking the Therapeutic Potential of Previously Undruggable GPCRs

    The significantly increased surface area of ligand-receptor interface for these GPCRs makes modulation Significant resources have been invested into the search for small molecule modulators of small protein important feature of Orion’s discovery process is that the initial search for potent target receptor modulators Orion’s receptor antagonist analogs have demonstrated powerful efficacies across a range of animal models Orion’s superagonist analogs are not only powerful candidate drugs for receptor modulation in indications

  • GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for...

    Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor "Modulators Herein, we demonstrate that a thiophene modification at the C8 position in the common adenine scaffold

  • Ode to GPCRs

    Our understanding of how various factors, such as lipid composition, osmotic stress, and allosteric ligands , modulate the conformational dynamics of GPCRs remains crude. Interaction of G-Protein βγ Complex with Chromatin Modulates GPCR- Dependent Gene Regulation.

  • Purpose-Driven Opioid Research: Catherine Demery’s Academic Path

    she collaborates with harm-reduction groups such as the Red Project in Grand Rapids  to ground her models This approach makes her models not just rigorous, but translational—bridging the gap between receptor Her next steps include using floxed mouse models  and viral tools  to dissect the downstream pathways Real-world data should guide how we build preclinical models. That urgency, more than titles, positions, or prestige, is what sustains a lasting career in science.

  • Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling

    subfamilies such as Gs, Gi/o, Gq/11, and G12/13, which orchestrate downstream signaling events, including the modulation cost of reagents, optimizing sensor expression levels and adapting these systems to disease-relevant models Addressing these hurdles is essential for translating findings from cellular models to clinically relevant development of the BERKY and the ONE-GO biosensors, designed to facilitate their application in disease models

  • Co-activation of GPCRs facilitate GIRK-dependent current

    The heterologous facilitation was modelled based on the known cooperative interaction between the G protein KEY POINTS: Inhibitory D2 and GABAB receptors modulate dopamine neuron activity through shared G protein-coupled

  • Is Your Agonist Really “Working”—Or Are You Just Seeing What Your System Allows?

    In this eye-opening module, Terry Kenakin explores a concept that could change how you interpret pharmacological

  • Navigating the Signaling Network: RTK and GPCR Crosstalk Uncovered

    Recently, Suchismita Roy et al. have explored how growth factors can modulate canonical G protein signaling primary research question addressed in this study was: How do growth factors, specifically through RTKs, modulate The ability of growth factors to modulate G protein signaling through specific phosphorylation events inform the development of therapeutic strategies aimed at targeting specific phosphorylation events to modulate

  • 📰 GPCR Weekly News, January 1 to 7, 2024

    ortholog MRGPRB2 Metabolite-sensing GPCRs in rheumatoid arthritis Dissecting the molecular basis for the modulation protein-coupled receptor Methods & Updates in GPCR Research RediscMol: Benchmarking Molecular Generation Models leucine and isoleucine in tuning the hydropathy of class A GPCRs Arylsulfatases and neuraminidases modulate

  • Latrophilin-1 drives neuron morphogenesis and shapes chemo- and mechanosensation-dependent ...

    Detailed expression and RNA-Seq analyses revealed specific LAT-1-positive neurons and first insights into the genetic network that is modulated by the receptor function.

  • 📰 GPCR Weekly News, January 8 to 14, 2024

    GPCRs in Neuroscience The Na+ leak channel NALCN controls spontaneous activity and mediates synaptic modulation learning Industry News Exscientia Unveils MolFlux: Empowering the ML Community in Molecular Predictive Modelling Executive Officer Unraveling GPCRs Conformations: A Leap in Drug Discovery with STAGS Machine Learning Model Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs NEW Senior Researcher in Structural Biology NEW Post-Doctoral

  • Profiling Immune Cell and Platelet Transcriptomes

    The identification of a diverse array of GPCRs in immune cells underscores their potential roles in modulating expression of chemokine receptors in monocytes and macrophages suggest that these GPCRs could be targeted to modulate

  • The Truth About GPCR Product Launches: Years in the Making

    a pattern emerged: some scaffolds showed dual responsiveness to pH through lifetime and brightness modulation (chemistry) → Discovery of pH-sensitive dual response (brightness + lifetime) → Application to GPCR models

  • 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 Homology modeling relies on using the known structure of a homologous protein as a template to model For proteins with low sequence similarity to available templates, homology models tend to be less accurate targeting TAAR1, more than double that of the homology models. Ligand discovery from a dopamine D3 receptor homology model and crystal structure.

  • Antibodies That Don’t Block, They Activate: A New Angle on Autoimmunity and GPCRs

    where this system is not just used for detection, but for functional screening : add ligands, track modulation

  • Why Mastering Pharmacokinetics Fundamentals Still Defines Discovery Success Today

    Kenakin argues, every downstream variable becomes distorted —from preclinical modeling to dose selection empowers chemists to optimize safety or PK without sacrificing target engagement Optimization should be modular mismatches between scaffold properties and biological surfaces Distribution: Beyond a Uniform Fluid Model compounds en route to renal excretion Species differences complicate translation from preclinical models Continuous PK integration —from scaffold design through population modeling— correlates with clinical

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