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Results found for "positive allosteric modulators"
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
CXCR1/2 inhibitors show beneficial effects in various animal models of CVD.
- Multifunctional role of GPCR signaling in epithelial tube formation
Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent
- Multifunctional role of GPCR signaling in epithelial tube formation
Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent
- Location bias contributes to functionally selective responses of biased CXCR3 agonists
In a mouse model of contact hypersensitivity, β-arrestin-biased CXCR3-mediated inflammation is dependent
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
We discuss the importance of understanding the translatability of cell and animal models to have more
- Adhesion GPCR Consortium Newsletter - May 2024
the afferent spiral ganglion neurons in the mouse cochlea where it localizes AMPA receptors at the post-synaptic : 38758649 Member Simone Prömel’s lab shows that the nematode (C. elegans) homolog of CELSR, FMI-1, modulates
- Orion Announces The Rapid Lead Optimization Of Ob-004 - A Ccr2 Antagonist
company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality
- A new Kunitz-type snake toxin family associated with an original mode of interaction with the...
Sequence comparison between active and non-active V2R Kunitz peptides highlighted five positions, among We finally determined that eight positions, part of these two loops, interact with the V2R.
- Phosphorylation of RGS regulates MAP kinase localization and promotes completion of cytokinesis
These data lead us to a model where Kel1 promotes completion of cytokinesis before pheromone-induced
- Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools
The reagents are compatible with HTRF readers and validated in GLP1R and Mu opioid receptor (MOR) models
- The Hidden Burn: How Internal Misalignment Drains Your Biotech’s Runway
. 👉 This post breaks down how biotech misalignment happens, what it costs you, and how to fix it before Example: Your platform team is building a modular assay framework. complete preclinical package by Q3.”Then it became “optimize lead series.”Then “refine bioavailability model
- Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in ...
In this study, we established an experimental Sjögren's syndrome (ESS) mouse model to elucidate the molecular increased saliva flow, alleviated salivary gland indices, and improved tissue integrity in the ESS model
- The Adhesion GPCR VLGR1/ADGRV1 Regulates the Ca2+ Homeostasis at Mitochondria-Associated ER Membrane
The absence of VLGR1 in tissues and cells derived from VLGR1-deficient mouse models resulted in alterations
- Breaking the Myth of High and Low Affinity Sites
Are You Using Models That Slow You Down?
- Novo Nordisk moves to strengthen obesity efforts
January 2022 "After securing FDA approval for Wegovy last year, Novo Nordisk is strengthening its position
- Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epith
Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the
- Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation
- Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone...
Moreover, the main investigations into animal models and ongoing clinical trials using these unimolecular
- Molecular basis for variations in the sensitivity of pathogenic rhodopsin variants to 9-cis-retinal
Nevertheless, estimates from computational modeling suggest that many of the least sensitive variants
- Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling
The structures reveal distinctive ligand engaging model and activation conformations of GPR110.
- Effect Delta-9-tetrahydrocannabinol and cannabidiol on milk proteins and lipid levels in HC11 cells
protein expression of major milk protein and lipid synthesizing markers. using the HC11 cells as a model
- 📰 GPCR Weekly News, October 30 to November 4, 2023
activation and to relieve neuropathic pain GPCRs in Oncology and Immunology Systems Pharmacodynamic Model natural products for specific, testosterone-like, OXER1 antagonists A 19F-qNMR-Guided Mathematical Model Cytokines GPCR Jobs NEW Research Scientist/Postdoctoral Associate in Computational Chemistry/Biophysics NEW Post-Doctoral
- Arginine 125 Is an Essential Residue for the Function of MRAP2
The aim of this work was to analyze the functional role of the specific arginine residue at position
- Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex
It reveals an atypical position of β-arrestin1 compared to previously described GPCR-arrestin assemblies
- How a Failed Experiment Created a Powerful GPCR Imaging Tool
Tissue responses defied the model.
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
Much of the understanding of psychedelic pharmacology is derived from rodent models, but most of this
- GPCR Happy Hour – Boston, Sept 2025
the discovery process, including its pioneering organellar electrophysiology platform, iPSC-derived models
- The microglial endocannabinoid system similarly regulated by lipopolysaccharide and interferon gamma
Microglia are one of few cell types with a self-contained endocannabinoid system and are positioned at
- Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR..
All molecular components (bosentan, hETB, membrane, and solvent) were represented with an all-atom model
- Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy...
described in the present study showed increased symptoms under methylphenidate treatment but responded positively






