Results 121 to 130 of about 1,298 (145)
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Luminogenic HiBiT Peptide-Based NanoBRET Ligand Binding Assays for Melatonin Receptors
ACS Pharmacology and Translational Science, 2022The two human melatonin receptors MT1 and MT2, which belong to the G protein-coupled receptor (GPCR) family, are important drug targets with approved indications for circadian rhythm- and sleep-related disorders and major depression. Currently, most of the pharmacological studies were performed using [3H]melatonin and 2-[125I]iodomelatonin (2-[125I ...
Rachel Friedman Ohana +2 more
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Single-Cell NanoBRET Imaging with Green-Range HaloTag Acceptor
2022Bioluminescence resonance energy transfer (BRET) has gained impetus to monitor protein interactions in proximity. BRET involves the energy transfer from a bioluminescent donor (luciferases) to a fluorescent acceptor. Since bioluminescence is an intrinsic phenomenon, BRET excludes the need for external illumination and serves as a powerful alternative ...
Ovia, Thirukkumaran, Hideaki, Mizuno
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Use of NanoBiT and NanoBRET to characterise interleukin‐23 receptor dimer formation in living cells
British Journal of Pharmacology, 2023 Background and PurposeInterleukin‐23 (IL‐23) and its receptor are important drug targets for the treatment of auto‐inflammatory diseases. IL‐23 binds to a receptor complex composed of two single transmembrane spanning proteins IL23R and IL12Rβ1. In this study, we aimed to gain further understanding of how ligand binding induces signalling of IL‐23 ...
Laura Kilpatrick, Stephen Hill
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Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET
International Journal of Molecular SciencesNanoLuc-mediated bioluminescence resonance energy transfer (NanoBRET) has gained popularity for its ability to homogenously measure ligand binding to G protein-coupled receptors (GPCRs), including the subfamily of chemokine receptors. These receptors, such as ACKR3, CXCR4, CXCR3, play a crucial role in the regulation of the immune system, are ...
Henry Vischer +2 more
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Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands
Bioconjugate Chemistry, 2019A critical part of the development of CXCR4 modulators is to have a simple and sensitive assay system to complement the search by screening and evaluating the binding affinity. Herein, a NanoBRET assay system was developed, and its feasibility as a high-throughput screening tool for potent CXCR4 ligands was ascertained.
Maxwell M. Sakyiamah +3 more
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Development of a Highly Selective NanoBRET Probe to Assess MAGL Inhibition in Live Cells
ChemBioChemAbstractCell‐free enzymatic assays are highly useful tools in early compound profiling due to their robustness and scalability. However, their inadequacy to reflect the complexity of target engagement in a cellular environment may lead to a significantly divergent pharmacology that is eventually observed in cells.
Luca Gobbi, Marc Nazare, Bernd Kuhn
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Measuring the rapid kinetics of receptor-ligand interactions in live cells using NanoBRET
2021The importance of receptor-ligand binding kinetics has often been overlooked during drug development, however, over the past decade it has become increasingly clear that a better understanding of the kinetic parameters is crucial for fully evaluating pharmacological effects of a drug.
Anna, Suchankova +2 more
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One Tracer, Dual Platforms: Unlocking Versatility of Fluorescent Probes in TR-FRET and NanoBRET Target Engagement Assays [PDF]
ACS Medicinal Chemistry LettersJin Wang, Xiaoli Qi
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ChemMedChemAbstractA conserved intracellular allosteric binding site (IABS) was recently identified at several G protein‐coupled receptors (GPCRs). This target site allows the binding of allosteric modulators and enables a new mode of GPCR inhibition. Herein, we report the development of a NanoBRET‐based assay platform based on the fluorescent ligand LT221 (5 ...
Matthias Schiedel +2 more
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Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells
2021Heterobifunctional small-molecule degraders known as Proteolysis Targeting Chimeras (PROTACs) serve as a chemical bridge bringing into direct association a target protein with an active E3 ligase complex, called the ternary complex, to facilitate targeted protein degradation. This ternary complex formation is the first key mechanistic step in a cascade
Sarah D, Mahan +3 more
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