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

Povzetek

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.

Ključne besede

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

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
UDK: 615.015.8
COBISS: 204113923 Povezava se bo odprla v novem oknu
ISSN: 2079-6382
Št. ogledov: 380
Št. prenosov: 73
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarni jezik: Slovenski jezik
Sekundarne ključne besede: avtolizin E;glikozid hidrolaza;iminosladkorji;površinska plazmonska resonanca;zaviranje encimov;Bakterijska rezistenca;
Vrsta dela (COBISS): Članek v reviji
Strani: str. 1-12
Letnik: ǂVol. ǂ13
Zvezek: ǂiss. ǂ8, [article no.] 751
Čas izdaje: 2024
DOI: 10.3390/antibiotics13080751
ID: 24720508