Janja Kocjan (Author), Tihomir Tomašić (Author), Marko Anderluh (Author), Martina Hrast (Author), Gregor Bajc (Author), Alen Sevšek (Author), Nathaniel I. Martin (Author), Roland J. Pieters (Author), Marjana Novič (Author), Katja Venko (Author)

Abstract

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 KD of 19 μM. The KD value for compound 8 was 88 μM, while compound 3 had a KD value of 410 μM.

Keywords

autolysin E;glycoside hydrolase;iminosugars;surface plasmon resonance;enzyme inhibition;

Data

Language: English
Year of publishing:
Typology: 1.01 - Original Scientific Article
Organization: UL FFA - Faculty of Pharmacy
UDC: 615.015.8
COBISS: 204113923 Link will open in a new window
ISSN: 2079-6382
Views: 380
Downloads: 73
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Other data

Secondary language: Slovenian
Secondary keywords: avtolizin E;glikozid hidrolaza;iminosladkorji;površinska plazmonska resonanca;zaviranje encimov;Bakterijska rezistenca;
Type (COBISS): Article
Pages: str. 1-12
Volume: ǂVol. ǂ13
Issue: ǂiss. ǂ8, [article no.] 751
Chronology: 2024
DOI: 10.3390/antibiotics13080751
ID: 24720508