Using a NanoBRET‐Based Ligand‐Binding Assay at the β2‐Adrenoceptor for Undergraduate Pharmacology Education [PDF]
Pharmacology Research & PerspectivesThe teaching of pharmacology includes a fundamental understanding of ligand binding; how it is measured and how it is calculated. We sought to modernize the techniques by which ligand affinity is determined by undergraduate students and introduce them to
Abigail Pearce +10 more
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NanoBRET in C. elegans illuminates functional receptor interactions in real time [PDF]
BMC Molecular and Cell Biology, 2022 Background Protein-protein interactions form the basis of every organism and thus, investigating their dynamics, intracellular protein localization, trafficking and interactions of distinct proteins such as receptors and their ligand-binding are of ...
Victoria Elisabeth Groß +4 more
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Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET [PDF]
iScience, 2018 Summary: The therapeutic action of a drug depends on its ability to engage with its molecular target in vivo. However, current drug discovery strategies quantify drug levels within organs rather than determining the binding of drugs directly to their ...
Diana C. Alcobia +9 more
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NanoBRET Tracer Development for Class I Bromodomain Target Engagement in Live Cells. [PDF]
Bioconjug ChemABSTRACT Epigenetic reader proteins, such as bromo-domains, are often associated with diseases such as cancer and inflammation. BET bromodomain inhibitors have been studied extensively; however, non-BET bromodomains are understudied.
Sneddon MS +4 more
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Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis [PDF]
iScience, 2019 Summary: The peptide hormone H2 relaxin has demonstrated promise as a therapeutic, but mimetic development has been hindered by the poorly understood relaxin receptor RXFP1 activation mechanism.
Bradley L. Hoare +8 more
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A Live-Cell NanoBRET Assay to Monitor RNA–Protein Interactions and Their Inhibition by Small Molecules [PDF]
ACS Central ScienceRNA-protein interactions are critical for cellular processes, including translation, pre-mRNA splicing, post-transcriptional modifications, and RNA stability. Their dysregulation is implicated in diseases such as myotonic dystrophy type 1 (DM1) and amyotrophic lateral sclerosis (ALS).
Jingsong Shan +8 more
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Development of a novel NanoBRET high-throughput drug screening assay for human GnRH receptor using sulfo-cyanine 5 fluorophore [PDF]
Journal of Pharmaceutical AnalysisG protein-coupled receptors (GPCRs), the largest superfamily of cell surface receptors and targets for over 30% of current clinical drugs, remain crucial for future therapeutic development.
Li Shen +8 more
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Development of a Lysine-Reactive Targeted Covalent Inhibitor for the P300/CBP-Associated Factor Bromodomain Through Structure-Based Design. [PDF]
ChemMedChemWe developed a targeted covalent inhibitor for the p300/CBP‐associated factor (PCAF) bromodomain. Our lead molecule, 10, labeled a unique lysine residue in the PCAF bromodomain, demonstrated potent inhibition in biophysical/biochemical assays, and engaged the PCAF bromodomain in cells.
Ede RR +9 more
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NanoBRET-based detection of ligand-receptor interactions at the neuropeptide FF receptor 1. [PDF]
RSC AdvCharacterization of ligand binding at the neuropeptide FF receptor 1 (NPFFR1) through a nanoBRET-based assay.
Lentschat H, Beck-Sickinger AG.
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Proximity labeling reveals non-catalytic interactions between DPP9 and ubiquitin signaling complexes [PDF]
Cellular and Molecular Life SciencesDipeptidyl peptidase 9 (DPP9) is an amino-peptidase with roles in immunity, DNA-repair, cell signaling, memory and neonatal survival; its dysregulation is linked to cancer and immune-related disorders.
Valentina Elena Wirtgen +10 more
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