Results 131 to 140 of about 1,298 (145)
NanoBRET ligand binding at a GPCR under endogenous promotion facilitated by CRISPR/Cas9 genome editing [PDF]
Cellular Signalling, 2019 Bioluminescence resonance energy transfer (BRET) is a versatile tool used to investigate membrane receptor signalling and function. We have recently developed a homogenous NanoBRET ligand binding assay to monitor interactions between G protein-coupled receptors and fluorescent ligands. However, this assay requires the exogenous expression of a receptor
Elizabeth Johstone +2 more
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Analytical Chemistry, 2022
By fusing several environment-sensitive fluorophores to the pharmacophore mirabegron, a series of new fluorescent ligands for β-adrenergic receptors (β-ARs) were produced with a turn-on mechanism and high binding affinity to β-ARs efficiently. Compound L5 with the pyridinium moiety possessed the most favorable combination of properties after systematic
Wenhua Li +5 more
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By fusing several environment-sensitive fluorophores to the pharmacophore mirabegron, a series of new fluorescent ligands for β-adrenergic receptors (β-ARs) were produced with a turn-on mechanism and high binding affinity to β-ARs efficiently. Compound L5 with the pyridinium moiety possessed the most favorable combination of properties after systematic
Wenhua Li +5 more
openaire +2 more sources
NanoBRET™ Live-Cell Kinase Selectivity Profiling Adapted for High-Throughput Screening
2023Kinases represent one of the most therapeutically tractable targets for drug discovery in the twenty-first century. However, confirming engagement and achieving intracellular kinase selectivity for small-molecule kinase inhibitors can represent noteworthy challenges.
Amanda N, Nieman +6 more
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Quantitative insights into protein turnover and ubiquitination with HiBiT and NanoBRET
Protein turnover and ubiquitination are fundamental processes regulating cellular homeostasis, proteostasis, and targeted protein degradation. Here, we present an optimized methodology for studying protein stability, ubiquitination dynamics, and degron function using HiBiT (11-amino-acid peptide tag) and NanoBRET (bioluminescence resonance energy ...Małgorzata, Piechota +1 more
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NanoBRET-Based Biosensor for High-Throughput Screening of RAB11A–FIP2 Interaction Inhibitors
Analytical ChemistryProtein-protein interactions (PPIs) are critical regulators of cellular processes and represent promising therapeutic targets. However, existing drug discovery approaches for PPI targeting, such as surface plasmon resonance, have inherent limitations, including their inability to fully recapitulate the cellular environment. To address these challenges,
Gaeun Yoo +5 more
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NanoBRET – ein neues Nachweisverfahren für die GPCR-Ligandenbindung
BIOspektrum, 2016A number of assay techniques are currently used to study ligand binding to G protein-coupled receptors (GPCRs) in living cells. In contrast to FRET, BRET does only need the addition of a suitable substrate to generate light/energy which then excites the fluorescent binding partner.
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Abstract 3512: Measuring intracellular target engagement and drug residence time with nanoBRET
Cancer Research, 2015Abstract We present a biophysical method to directly measure target engagement within intact mammalian cells using bioluminescence energy transfer (BRET). Compound interactions with intracellular targets can be detected with complete specificity by their ability to compete with energy transfer complexes introduced into the cells.
Matthew B. Robers +12 more
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NanoBRET to probe ligand-receptor and receptor-receptor interactions in living cells
2019This thesis describes a novel technique known as NanoBRET to monitor direct binding of a drug to its cognate receptor in living mice. It also describes the application of this technology to investigate interactions between two major transmembrane receptor proteins, namely Vascular endothelial receptor 2 (VEGFR2) and β2-adrenoceptor.
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