20.500.12556/RUL-138728 DNA-encoded library screening on two validated enzymes of the peptidoglycan biosynthetic pathway 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. antibacterial agents DNA-encoded library screening inhibitors antibakterijska sredstva DNA-kodirana knjižnica inhibitorji true false true Angleški jezik Slovenski jezik Članek v reviji 2022-08-11 07:11:34 2022-08-11 07:11:42 2022-09-15 04:17:06 0000-00-00 00:00:00 2022 0 0 4 str. art. 128915 Vol. 73 2022 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 615.4.54 0960-894X 10.1016/j.bmcl.2022.128915 117813507 1-s2.0-S0960894X22003912-main.pdf 1-s2.0-S0960894X22003912-main.pdf 1 590EA3D73D8DBFCC466C6D9207E8DBEB eefab35a0ef8141ec115c9123ccdc73e3cc643120d7fc2aecfb5abc3241a3579 fd1fdb15-2e81-11ed-92af-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=160414 https://www.sciencedirect.com/science/article/pii/S0960894X22003912 1 cba0d925-1933-11ed-8aca-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=159150 Fakulteta za farmacijo 0 0 0