ArticleAngewandte Chemie (International ed. in English)2021
The Development of a Fluorescence-Based Competitive Assay Enabled the Discovery of Dimeric Cyclic Peptide Modulators of Ubiquitin Chains.
Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Catalytic thiolation-depolymerization-like decomposition of oxyphenylene-type super engineering plastics via selective carbon-oxygen main chain cleavages.Communications chemistry · 2024Article
- Combining Chemical Protein Synthesis and Random Nonstandard Peptides Integrated Discovery for Modulating Biological Processes.Accounts of chemical research · 2023Article
- Selective macrocyclic peptide modulators of Lys63-linked ubiquitin chains disrupt DNA damage repair.Nature communications · 2022Article
- Gold(I)-Mediated Rapid Cyclization of Propargylated Peptides via Imine Formation.Journal of the American Chemical Society · 2022Article
- Highly Efficient Cyclization Approach of Propargylated Peptides via Gold(I)-Mediated Sequential C-N, C-O, and C-C Bond Formation.ACS central science · 2021Article
- The Development of a Fluorescence-Based Competitive Assay Enabled the Discovery of Dimeric Cyclic Peptide Modulators of Ubiquitin Chains.Angewandte Chemie (International ed. in English) · 2021Article
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Authors and funding
5 authors.
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Abstract
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 tetraubiquitin chain in a relatively simple, fast, and affordable manner. This approach combined with a state-of-the-art toolbox of chemical protein synthesis and a specially optimized Cys deprotection protocol enabled us to design highly potent, Lys48-linked tetraubiquitin chain selective "next generation" dimeric peptide modulators. The dimeric peptide exhibited cancer cell permeability and induced cell death with higher efficiency compared to its monocyclic analogue. These features make our dimeric peptide a promising candidate for further studies using in vivo models. Our assay can be adopted for other various ubiquitin chains in their free or anchored forms as well as conjugates for Ub-like modifiers.
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