Počet záznamů: 1
Mapping the Pro-Peptide of the Schistosoma mansoni Cathepsin B1 Drug Target: Modulation of Inhibition by Heparin and Design of Mimetic Inhibitors
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SYSNO ASEP 0360455 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Mapping the Pro-Peptide of the Schistosoma mansoni Cathepsin B1 Drug Target: Modulation of Inhibition by Heparin and Design of Mimetic Inhibitors Tvůrce(i) Horn, Martin (UOCHB-X) RID, ORCID
Jílková, Adéla (UOCHB-X) RID, ORCID
Vondrášek, Jiří (UOCHB-X) RID, ORCID
Marešová, Lucie (UOCHB-X) RID
Caffrey, C. R. (US)
Mareš, Michael (UOCHB-X) RID, ORCIDCelkový počet autorů 6 Zdroj.dok. ACS Chemical Biology. - : American Chemical Society - ISSN 1554-8929
Roč. 6, č. 6 (2011), s. 609-617Poč.str. 9 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova Schistosoma mansoni ; cathepsin B ; propeptide Vědní obor RIV CE - Biochemie CEP GA203/09/1585 GA ČR - Grantová agentura ČR KJB400550516 GA AV ČR - Akademie věd IAA400550705 GA AV ČR - Akademie věd CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000291896400011 DOI 10.1021/cb100411v Anotace Blood flukes of the genus Schistosoma cause the disease schistosomiasis that infects over 200 million people worldwide. Schistosoma mansoni cathepsin B1 (SmCB1) is a gut-associated protease that digests host blood proteins as source of nutrients. Enzymatic activity of the SmCB1 zymogen is prevented by the pro-peptide that sterically blocks the active site until activation of the zymogen to the mature enzyme. We investigated the structure-inhibition relationships of how the SmCB1 pro-peptide interacts with the enzyme core using a SmCB1 zymogen model and pro-peptide-derived synthetic fragments. Two regions were identified within the pro-peptide that govern its inhibitory interaction with the enzyme core: an 'active site region' and a unique 'heparin-binding region' that requires heparin. Using the active site region as a template and a docking model of SmCB1, we designed a series of inhibitors mimicking the pro-peptide structure. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2012
Počet záznamů: 1