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doi:10.22028/D291-30948
Title: | Phage Display on the Anti-infective Target 1-Deoxy-d-xylulose-5-phosphate Synthase Leads to an Acceptor-Substrate Competitive Peptidic Inhibitor |
Author(s): | Marcozzi, Alessio Masini, Tiziana Zhu, Di Pesce, Diego Illarionov, Boris Fischer, Markus Herrmann, Andreas Hirsch, Anna |
Language: | English |
Title: | ChemBioChem : a European journal of chemical biology |
Volume: | 19 |
Issue: | 1 |
Startpage: | 58 |
Endpage: | 65 |
Publisher/Platform: | Wiley-VCH |
Year of Publication: | 2018 |
Publikation type: | Journal Article |
Abstract: | Enzymes of the 2-C-methyl-d-erythritol-4-phosphate pathway for the biosynthesis of isoprenoid precursors are validated drug targets. By performing phage display on 1-deoxy-d-xylulose-5-phosphate synthase (DXS), which catalyzes the first step of this pathway, we discovered several peptide hits and recognized false-positive hits. The enriched peptide binder P12 emerged as a substrate (d-glyceraldehyde-3-phosphate)-competitive inhibitor of Deinococcus radiodurans DXS. The results indicate possible overlap of the cofactor- and acceptor-substrate-binding pockets and provide inspiration for the design of inhibitors of DXS with a unique and novel mechanism of inhibition. |
DOI of the first publication: | 10.1002/cbic.201700402 |
URL of the first publication: | https://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/cbic.201700402 |
Link to this record: | hdl:20.500.11880/29157 http://dx.doi.org/10.22028/D291-30948 |
ISSN: | 1439-7633 0044-8249 1439-4227 |
Date of registration: | 15-May-2020 |
Faculty: | NT - Naturwissenschaftlich- Technische Fakultät |
Department: | NT - Pharmazie |
Professorship: | NT - Prof. Dr. Anna Hirsch |
Collections: | SciDok - Der Wissenschaftsserver der Universität des Saarlandes |
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