20.500.12556/RUL-160064 Targeting N-acetylglucosaminidase in Staphylococcus aureus with iminosugar inhibitors Bacteria are capable of remarkable adaptations to their environment, including undesirable bacterial resistance to antibacterial agents. One of the most serious cases is an infection caused by multidrug-resistant Staphylococcus aureus, which has unfortunately also spread outside hospitals. Therefore, the development of new effective antibacterial agents is extremely important to solve the increasing problem of bacterial resistance. The bacteriolytic enzyme autolysin E (AtlE) is a promising new drug target as it plays a key role in the degradation of peptidoglycan in the bacterial cell wall. Consequently, disruption of function can have an immense impact on bacterial growth and survival. An in silico and in vitro evaluation of iminosugar derivatives as potent inhibitors of S. aureus (AtlE) was performed. Three promising hit compounds (1, 3 and 8) were identified as AtlE binders in the micromolar range as measured by surface plasmon resonance. The most potent compound among the SPR response curve hits was 1, with a K$_D$ of 19 μM. The K$_D$ value for compound 8 was 88 μM, while compound 3 had a K$_D$ value of 410 μM. autolysin E glycoside hydrolase iminosugars surface plasmon resonance enzyme inhibition avtolizin E glikozid hidrolaza iminosladkorji površinska plazmonska resonanca zaviranje encimov bakterijska rezistenca true false true Angleški jezik Slovenski jezik Članek v reviji 2024-08-14 09:50:33 2024-08-14 09:50:37 2025-01-31 13:48:24 0000-00-00 00:00:00 2024 0 0 12 str. iss. 8, art. 751 Vol. 13 2024 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 615.015.8 2079-6382 10.3390/antibiotics13080751 204113923 antibiotics-13-00751.pdf antibiotics-13-00751.pdf 1 8D429F08799F0CEBD3DD63A8006B1B24 510fd5758f786da8f92066a647d98ac899c4807fb72d04a843864a37633c9d0b b0e4cf43-5a14-11ef-8f74-0050569b8976 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=188495 https://www.mdpi.com/2079-6382/13/8/751 1 b9d7888b-5a11-11ef-8f74-0050569b8976 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=188494 Fakulteta za farmacijo Biotehniška fakulteta 0 0 0