SLAS TECHNOLOGY · 2023 · 12 citations · 8 references
PharmacyBiochemistryMedicinal ChemistryBiophysical ChemistryDrug DesignDrug DiscoveryHigh-throughput ScreeningLigand BindingMolecular ScreeningSmall-molecule ScreeningAffinity AssaysBiophysical AssaysDifferential Scanning FluorimetryHigh-throughput Screening AssaysLigand-binding AssaysMelting TemperatureMelting Temperature AnalysisThermal Shift Assays
Biophysical affinity screening is increasingly being adopted as a high-throughput hit finding technique in drug discovery. Automation is highly beneficial to high-throughput screening (HTS) since a large number of compounds need to be reproducibly tested against a biological target. Herein, we describe how we have automated two biophysical affinity screening methods that rely on a thermal shift in protein melting temperature upon small molecule binding: differential scanning fluorimetry (DSF) and the cellular thermal shift assay (CETSA).
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Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
Daniel Martinez Molina, Rozbeh Jafari, Marina Ignatushchenko et al. · Science · 2013 · 2.2K citations
Medicine, Oncology, Pharmacology +17
CRISPR-Mediated Tagging of Endogenous Proteins with a Luminescent Peptide
Marie K. Schwinn, Thomas Machleidt, Kris Zimmerman et al. · ACS Chemical Biology · 2017 · 455 citations · Full text