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351 items found for "cancer cell lines"
- Location bias contributes to functionally selective responses of biased CXCR3 agonists
In CD8 + T cells, the chemokines promote unique transcriptional responses predicted to regulate inflammatory
- Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs
Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest
- Job Opportunity Spotlight #1: Principal Scientist, In Vitro Pharmacology
Someone with strong assay development skills as well as strong data analysis and interpretation skills Beth: “We focus on biochemical, cell based, and radioligand binding assays to enable SAR, MOA, lead Top candidates will have a solid foundation in GPCR pharmacology as well as some experience in drug discovery Beth: “Well, I enjoy training and mentoring team members.
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
By means of these studies, we developed 14 as a fluorescent CCR2 ligand, enabling cell-free as well
- 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
- Therapeutic validation of an orphan G protein‐coupled receptor
functions, such as sensory perception, reproduction, development, growth, metabolism, and are also linked GPR84 is a Gi‐coupled class A GPCR mainly expressed in immune cells and microglia in the brain (Wojciechowicz Regarding the first question, GPR84 overexpression in immune cells in a range of pro‐inflammatory disorders In addition, several GPR84 ligands have been described as well as GPR84 knockout mice. the investment in better tools to study its function in both disease and physiological settings will likely
- Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent..
epitope-tagged GCGRs undergo clathrin- and dynamin-dependent endocytosis in HEK293 and Huh-7-Lunet cells
- Drug Discovery Picks Up the Pace, Stays on Target
small molecules that conditionally modulate proteins in their functional state; three-dimensional (3D) cell
- Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR..
ligand-receptor binding by searching large-scale motions accompanied with stable maintenance of the fragile cell-membrane The deepest basin in the resultant free-energy landscape was assigned to native-like complex conformation Eventually, the native-like complex is completed.
- Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its...
They participate in the activation, chemotaxis and recruitment of multiple immunological cells such as
- 📰 GPCR Weekly News, December 4 to 10, 2023
GPCR University live Zoom sessions hosted by Dr. Terry Kenakin. The package includes four live Zoom sessions, a one-year Dr. G protein signaling protein 6 alleviates acute lung injury by inhibiting inflammation and promoting cell neuroscience drugmaker Cerevel Therapeutics for $8.7 billion FDA approves two gene therapies for sickle cell
- Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System
vary between antagonist, partial agonist, and biased agonist outcomes in various primary and clonal cell We will discuss the historic context of pepducin development for each receptor, as well as the structural
- Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated
Here we investigated a potential mechanism for regulation of PLC signaling downstream of MOR in HEK293 cells
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
"Genetically encoded fluorescent biosensors allow intracellular signaling dynamics to be tracked in live cells and tissues using optical detection.
- 📰 GPCR Weekly News, February 19 to 25, 2024
We would like to extend our heartfelt thanks to Dr. We will be offering this live course again later this year. GPR3 After wounding, a G-protein coupled receptor promotes the restoration of tension in epithelial cells determines temperature acclimatization of Caenorhabditis elegan Species-Specific Duplicated FMRFaR-like glutamatergic neurons GPCRs in Oncology and Immunology TIPE proteins control directed migration of human T cells
- 📰 GPCR Weekly News, July 24 to July 30, 2023
Submit a 1-minute abstract video and tell us more about your project using this form. Intracellular calcium ion transients evoked by cell poking independently of released autocrine ATP in Madin-Darby canine kidney cells.
- Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
S1P5 is predominantly expressed in nervous and immune systems, regulating the egress of natural killer cells from lymph nodes and playing a role in immune and neurodegenerative disorders, as well as carcinogenesis
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
transduce signals across the plasma membrane and orchestrate a multitude of physiological processes within cells
- Molecular basis for variations in the sensitivity of pathogenic rhodopsin variants to 9-cis-retinal
September 2022 "Over 100 mutations in the rhodopsin gene have been linked to a spectrum of retinopathies previously uncharacterized variants, that exhibit diminished plasma membrane expression in HEK293T cells
- Precise druggability of the PTH type 1 receptor
selective small molecules with strong negative allosteric and biased properties for PTHR signaling in cell
- A Chemical Biology Toolbox Targeting the Intracellular Binding Site of CCR9: Fluorescent Ligands ...
first synthesized a fluorescent ligand enabling equilibrium and kinetic binding studies via NanoBRET as well Applying this molecular tool in a membrane-based setup and in living cells, we discovered a 4-aminopyrimidine
- 📰 GPCR Weekly News, May 27 to June 2, 2024
Badr Sokrat is live! You can now watch podcast episodes in video format on our website. regulates the expression and alternative splicing of genes associated with aphasia-related diseases in PC12 cells asthma GPCR Events, Meetings, and Webinars June 2 - 7, 2024 | Chemotactic Cytokines June 4, 2024 | Live Scientist Senior Research Associate/Associate Scientist, Protein Science Post-Doctoral Fellow—Pharmacology/Cell
- Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental...
endoplasmic reticulum stress, dysregulated immune tolerance, vascular inflammation and endothelial cell
- Design and validation of recombinant protein standards for quantitative Western blot analysis of...
recombinant protein standards for quantitative Western blot analysis of cannabinoid CB1 receptor density in cell
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
depression was involved in the biological process of GPCR signal transduction, hormone metabolism and nerve cell
- 📰 GPCR Weekly News, February 5 to 11, 2024
We will be offering this live course later this year. GPCRs in Cardiology, Endocrinology, and Taste G protein-coupled receptors driven intestinal glucagon-like News Exscientia Initiates Clinical Study to Further Evaluate Functional Precision Medicine Platform in Cancer
- 📰 GPCR Weekly News, July 1 to 7, 2024
of dynamic cAMP responses to GPCR agonists for exploration of GLP-1R ligand effects in pancreatic β-cells blockers GPCR Events, Meetings, and Webinars September 18, 2024 | FREE Webinar - The value of GPCR cell-based
- The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in ...
In ascomycete fungi including yeasts, mating between cells of opposite mating type depends on the molecular Although such pheromone/receptor systems are likely to function in both mate choice and prezygotic isolation