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- Structure of Mycobacterium tuberculosis Cya, an evolutionary ancestor of the mammalian membrane...
tuberculosis adenylyl cyclase (AC) Rv1625c/Cya is an evolutionary ancestor of the mammalian membrane ACs and a model
- 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
- 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
- How GPCR Spatial Signaling Sparked a Scientific Journey
Her early work didn’t involve groundbreaking receptor models or million-dollar grants.
- 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
- Molecular creativity in drug discovery
. • Training Builds Innovation : Her lab model at Monash is shaping the next generation of GPCR scientists
- 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
- How Fast Does a Drug Work?
Don’t Let Outdated Models Slow Your Next Program The analytical tools that shaped traditional affinity
- GPCRs at Discovery on Target 2026
states of the receptor, and the weak partial agonist still delivered meaningful pain relief in a mouse 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
- 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
- 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
- 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
- đź“° GPCR Weekly News, October 30 to November 4, 2023
guanine-nucleotide exchange factor RIC-8 regulates cilia morphogenesis in Caenorhabditis elegans sensory neurons 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
- GPCR Updates: Celebrating Breakthroughs, New Course Launches Soon, and Exclusive Discounts! | Aug 26 - Sep 1, 2024
Treasures Edelris Announces Research Services Agreement with Pfizer on Targeted Protein Degradation Modalities the cleavage of the porcine embryo by regulating HSP90 and the AKT pathway Structural basis for CCR6 modulation dimer mGlu5 Altered O-glycosylation of β1-adrenergic receptor N-terminal single-nucleotide variants modulates
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
A High Content Screening focused microscope that has a confocal-like mode as well. receptor localization in defined states (pharmacological stimulation, genetic modification, disease models
- 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
- 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
- GPCRs are not simple on-off switches: deep dive into GPCR-ligand interactions
An alternative and promising approach is allosteric modulation. Over the past decade, there has been a notable growth in the discovery of allosteric modulators for GPCRs which possess the capability to modulate and fine-tune the affinity and/or efficacy of orthosteric ligands Allosteric modulators that do not exhibit agonistic properties remain inactive in the absence of endogenous In this context, allosteric modulators exhibiting constrained positive or negative cooperativity are
- 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
- Unlock the Hidden Complexity Behind GPCRs—From Terry Kenakin’s Vault
With insights from molecular dynamics, biased signaling, and allosteric modulation, this session lays
- 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 landscape of the Chemokine Receptor system
Chemokine Binding Mode – from CRS1 to CRS3 Chemokines possess a conserved tertiary structure known as Chemokine-CKR interaction follows a common pattern which is generally described by the classic “two-site” model Biased Agonism – CCR1 as a model CKR Three active-state structures of CCR1 have been characterized, all signaling, which has been structurally related to a conformational change of Y2917.43 tilted toward TM2, a model The Non-canonical Toggle Switch 6.48 - CCR6 as a model CKR The structure of CCR6 bound to CCL20 reveals
- From Farm Fields to GPCR Discovery, GLP-1 and GIP
Studying the pancreatic islet — specifically the beta cells  that release insulin — offered a unique model GPCR–islet signaling links extended beyond classical ligand models.Collaboration and long-term persistence
- GPCR Internalization: When the Signal Moves Inside the Cell
The model needs to account for the possibility that both arms of the pharmacological response — activation
- 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.
- 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
- How Breakthroughs Happen: Eric Trinquet on Innovation, Serendipity & GPCRs
From probe solubility to photophysics, from tag strategies to model systems, every variable was debated
- 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











