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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|
|Title:||ChemBioChem : a European journal of chemical biology|
|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|
|Date of registration:||15-May-2020|
|Faculty:||NT - Naturwissenschaftlich- Technische Fakultät|
|Department:||NT - Pharmazie|
|Professorship:||NT - Prof. Dr. Anna Hirsch|
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