Results 1 to 10 of about 488 (104)
An Integrated Approach toward NanoBRET Tracers for Analysis of GPCR Ligand Engagement
Molecules, 2021 Gaining insight into the pharmacology of ligand engagement with G-protein coupled receptors (GPCRs) under biologically relevant conditions is vital to both drug discovery and basic research.
Rachel Friedman Ohana +1 more
exaly +4 more sources
Development of a NanoBRET assay for evaluation of 14-3-3σ molecular glues [PDF]
SLAS DiscoveryWe report the development of a 384-well formatted NanoBRET assay to characterize molecular glues of 14-3-3/client interactions in living cells. The seven isoforms of 14-3-3 are dimeric hub proteins with diverse roles including transcription factor ...
Markella Konstantinidou +2 more
exaly +4 more sources
Development of SYK NanoBRET cellular target engagement assays for gain–of–function variants [PDF]
Frontiers in Chemical BiologySpleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase that is activated by phosphorylation events downstream of FcR, B-cell and T-cell receptors, integrins, and C-type lectin receptors. When the tandem Src homology 2 (SH2) domains of SYK bind to
Matthew Robers +2 more
exaly +4 more sources
Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells [PDF]
Molecules, 2023 PLK1 is a protein kinase that regulates mitosis and is both an important oncology drug target and a potential antitarget of drugs for the DNA damage response pathway or anti-infective host kinases.
Xuan Yang +7 more
doaj +3 more sources
Protocol for measuring BRAF autoinhibition in live cells using a proximity-based NanoBRET assay
STAR Protocols, 2023 Summary: BRAF is frequently activated via mutation in human cancer and the RASopathy syndromes; however, for BRAF activation to occur, autoinhibitory interactions between the regulatory and catalytic domains must be relieved. Here, we present a proximity-
Russell Spencer-Smith +1 more
doaj +2 more sources
REGA-SIGN: Development of a Novel Set of NanoBRET-Based G Protein Biosensors
Biosensors, 2023 Despite G protein-coupled receptors (GPCRs) being important theapeutic targets, the signaling properties of many GPCRs remain poorly characterized. GPCR activation primarily initiates heterotrimeric G protein signaling. To detect ligand-induced G protein
Nathan Vanalken +2 more
exaly +3 more sources
NanoBRET: The Bright Future of Proximity-Based Assays
Frontiers in Bioengineering and Biotechnology, 2019 Bioluminescence resonance energy transfer (BRET) is a biophysical technique used to monitor proximity within live cells. BRET exploits the naturally occurring phenomenon of dipole-dipole energy transfer from a donor enzyme (luciferase) to an acceptor ...
Elizabeth Johstone +2 more
exaly +3 more sources
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
doaj +2 more sources
BRET measurement on CCD camera-based microtiter plate readers
SLAS Discovery, 2022 NanoBRET assays, which utilize bioluminescence energy resonance transfer (BRET), have been widely adopted in drug discovery for measuring both protein-protein interactions and drug target engagement. While the EnVision and other traditional well-scanning
Kelvin F. Cho +2 more
doaj +1 more source
Single tracer-based protocol for broad-spectrum kinase profiling in live cells with NanoBRET
STAR Protocols, 2021 Summary: This protocol is used to profile the engagement of kinase inhibitors across nearly 200 kinases in a live-cell context. This protocol utilizes one single kinase tracer (NanoBRET(TM) Tracer K10) that operates quantitatively at four different ...
Matthew B. Robers +5 more
doaj +1 more source