The Development of a Fluorescence‐Based Competitive Assay Enabled the Discovery of Dimeric Cyclic Peptide Modulators of Ubiquitin Chains

Development of modulators targeting specific interactions of ubiquitin‐based conjugates with their partners is a formidable task since it requires a suitable screening assay and homogeneous ubiquitin conjugates. We developed a novel high‐throughput strategy for screening ligands for Lys48‐linked tet...

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Veröffentlicht in:	Angewandte Chemie International Edition 2021-03, Vol.60 (13), p.7018-7023
Hauptverfasser:	Vamisetti, Ganga B., Meledin, Roman, Nawatha, Mickal, Suga, Hiroaki, Brik, Ashraf
Format:	Artikel
Sprache:	eng
Schlagworte:	Assaying Cell death Cell Death - drug effects Cell permeability Chains Chemical synthesis Chemistry Chemistry, Multidisciplinary Communication Communications Conjugates cyclic peptides dimeric peptides Dimers Dose-Response Relationship, Drug Drug Development Fluorescence fluorescence-based assay HeLa Cells high-throughput screening High-Throughput Screening Assays Humans In vivo methods and tests Ligands Modulators peptide engineering Peptides Peptides, Cyclic - chemical synthesis Peptides, Cyclic - chemistry Peptides, Cyclic - pharmacology Physical Sciences Protein biosynthesis Protein synthesis Science & Technology Screening Ubiquitin Ubiquitin - chemistry Ubiquitin - pharmacology
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