Aleš Žula (Avtor), Izabela Będziak (Avtor), Danijel Kikelj (Avtor), Janez Ilaš (Avtor)

Povzetek

Spumigins are marine natural products derived from cyanobacteria Nodularia spumigena, which mimics the structure of the D-Phe-Pro-Arg sequence and is crucial for binding to the active site of serine proteases thrombin and factor Xa. Biological evaluation of spumigins showed that spumigins with a (2S,4S)-4-methylproline central core represent potential lead compounds for the development of a new structural type of direct thrombin inhibitors. Herein, we represent synthesis and thrombin inhibitory activity of a focused library of spumigins analogues with indoline ring or L-proline as a central core. Novel compounds show additional insight into the structure and biological effects of spumigins. The most active analogue was found to be a derivative containing L-proline central core with low micromolar thrombin inhibitory activity.

Ključne besede

biokemija;morski proizvodi;naravni peptidi;inhibicija trombina;marine products;natural peptides;peptidomimetics;thrombin inhibition;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
Založnik: MDPI
UDK: 577
COBISS: 39787781 Povezava se bo odprla v novem oknu
ISSN: 1660-3397
Št. ogledov: 277
Št. prenosov: 148
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: biokemija;morski proizvodi;naravni peptidi;inhibicija trombina;
Vrsta dela (COBISS): Članek v reviji
Strani: str. 1-19
Letnik: ǂVol. ǂ16
Zvezek: ǂiss. ǂ11
Čas izdaje: Nov. 2018
DOI: 10.3390/md16110413
ID: 12639651