Please use this identifier to cite or link to this item: doi:10.22028/D291-30948
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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:UniBib – Die Universitätsbibliographie

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