The MALDI-TOF E2/E3 Ligase Assay as Universal Tool for Drug Discovery in the Ubiquitin Pathway

Due to their role in many diseases, enzymes of the ubiquitin system have recently become interesting drug targets. Despite efforts, primary screenings of compound libraries targeting E2 enzymes and E3 ligases have been strongly limited by the lack of robust and fast high-throughput assays. Here we r...

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Veröffentlicht in:	Cell chemical biology 2018-09, Vol.25 (9), p.1117-1127.e4
Hauptverfasser:	De Cesare, Virginia, Johnson, Clare, Barlow, Victoria, Hastie, James, Knebel, Axel, Trost, Matthias
Format:	Artikel
Sprache:	eng
Schlagworte:	Drug Discovery - methods Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology High-Throughput Screening Assays - methods Humans Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization - methods Ubiquitin - metabolism Ubiquitin-Conjugating Enzymes - antagonists & inhibitors Ubiquitin-Conjugating Enzymes - metabolism Ubiquitin-Protein Ligases - antagonists & inhibitors Ubiquitin-Protein Ligases - metabolism Ubiquitination - drug effects
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