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DNA-encoded library screening on two validated enzymes of the peptidoglycan biosynthetic pathwayProj, Matic ...Screening of DNA-encoded libraries is an emerging technology for discovering hits against protein targets. With the recent launch of the DELopen platform, a facile screening of 4.4 billion compounds ... is available to accelerate the drug discovery process. Here we report an affinity-based screening of the DELopen library for the first time. The screening was performed against two bacterial enzymes of the peptidoglycan biosynthetic pathway, Nacetylglucosamine- enolpyruvyl transferase (MurA) and D-alanine:D-alanine ligase (DdlB). Several binders were obtained and selected for off-DNA synthesis. Hits with confirmed inhibitory potency were deconstructed into smaller fragments. In this way, two new MurA inhibitors with antibacterial activity were obtained and are available for further optimization.Source: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 73, art. 128915, 2022, 4 str.)Type of material - article, component part ; adult, seriousPublish date - 2022Language - englishCOBISS.SI-ID - 117813507
Author | Proj, Matic ... |
Title | DNA-encoded library screening on two validated enzymes of the peptidoglycan biosynthetic pathway |
Publication date | 2022-07-30 |
COBISS.SI-ID | 117813507 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2022 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Razvoj protibakteriskih učinkovin z delovanjem na validirane tarče v biosintezi peptidoglikana | J1-2484-2020 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
Files that belong to the publication
Link |
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https://www.sciencedirect.com/science/article/pii/S0960894X22003912 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=138728 |
source: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 73, art. 128915, 2022, 4 str.)
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Database name | Field | Year |
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Proj, Matic | 52376 |
Bozovičar, Krištof | 53738 |
Hrast, Martina | 32036 |
Frlan, Rok | 26512 |
Gobec, Stanislav, 1970- | 15284 |
Source: Personal bibliographies
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