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DNA-encoded library screening on two validated enzymes of the peptidoglycan biosynthetic pathway
ID Proj, Matic (Author), ID Bozovičar, Krištof (Author), ID Hrast, Martina (Author), ID Frlan, Rok (Author), ID Gobec, Stanislav (Author)

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Abstract
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, N-acetylglucosamine-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.

Language:English
Keywords:antibacterial agents, DNA-encoded library, screening, inhibitors
Work type:Article
Typology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Publication status:Published
Publication version:Version of Record
Year:2022
Number of pages:4 str.
Numbering:Vol. 73, art. 128915
PID:20.500.12556/RUL-138728 This link opens in a new window
UDC:615.4.54
ISSN on article:0960-894X
DOI:10.1016/j.bmcl.2022.128915 This link opens in a new window
COBISS.SI-ID:117813507 This link opens in a new window
Publication date in RUL:11.08.2022
Views:401
Downloads:151
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Record is a part of a journal

Title:Bioorganic & medicinal chemistry letters
Shortened title:Bioorg. med. chem. lett.
Publisher:Elsevier
ISSN:0960-894X
COBISS.SI-ID:34486272 This link opens in a new window

Licences

License:CC BY 4.0, Creative Commons Attribution 4.0 International
Link:http://creativecommons.org/licenses/by/4.0/
Description:This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.

Secondary language

Language:Slovenian
Keywords:antibakterijska sredstva, DNA-kodirana knjižnica, inhibitorji

Projects

Funder:ARRS - Slovenian Research Agency
Project number:P1-0208
Name:Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin

Funder:ARRS - Slovenian Research Agency
Project number:J1-2484
Name:Razvoj protibakterijskih učinkovin z delovanjem na validirane tarče v biosintezi peptidoglikana

Funder:ARRS - Slovenian Research Agency
Funding programme:Young researchers

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