Use of NanoBiT and NanoBRET to characterise interleukin‐23 receptor dimer formation in living cells [PDF]
Background and Purpose: Interleukin-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.
Laura Kilpatrick, Stephen Hill
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Investigation of Receptor Heteromers Using NanoBRET Ligand Binding [PDF]
Receptor heteromerization is the formation of a complex involving at least two different receptors with pharmacology that is distinct from that exhibited by its constituent receptor units. Detection of these complexes and monitoring their pharmacology is
Elizabeth Johstone +2 more
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Luminogenic HiBiT Peptide-Based NanoBRET Ligand Binding Assays for Melatonin Receptors
The 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.
Rachel Friedman Ohana +2 more
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Development of NanoBRET‐Binding Assays for FKBP‐Ligand Profiling in Living Cells
FK506‐binding proteins (FKBPs) are promising targets for a variety of disorders and infectious diseases. High FKBP occupancy is thought to be necessary for ligands to effectively compete with the endogenous intracellular functions of FKBPs.
Felix Hausch, Jürgen Kolos
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Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET
NanoLuc-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.
Henry Vischer +2 more
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Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1 [PDF]
A 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
Matthias Schiedel +2 more
exaly +2 more sources
A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor [PDF]
There is a growing interest in understanding the binding kinetics of compounds that bind to G proteincoupled receptors prior to progressing a lead compound into clinical trials.
Stephen Briddon +2 more
exaly +2 more sources
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Measuring the rapid kinetics of receptor-ligand interactions in live cells using NanoBRET
Methods in Cell Biology, 2021Graham Ladds, Matt Harris
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NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs
Trends in Pharmacological Sciences, 2018Laura Kilpatrick +2 more
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