Počet záznamů: 1

Structural Basis for Inhibition of Cathepsin B Drug Target from the Human Blood Fluke, Schistosoma mansoni

  1. 1.
    0365166 - UOCHB-X 2012 RIV US eng J - Článek v odborném periodiku
    Jílková, Adéla - Řezáčová, Pavlína - Lepšík, Martin - Horn, Martin - Váchová, Jana - Fanfrlík, Jindřich - Brynda, Jiří - McKerrow, J. H. - Caffrey, C. R. - Mareš, Michael
    Structural Basis for Inhibition of Cathepsin B Drug Target from the Human Blood Fluke, Schistosoma mansoni.
    Journal of Biological Chemistry. Roč. 286, č. 41 (2011), s. 35770-35881 ISSN 0021-9258
    Grant CEP: GA ČR GA203/09/1585; GA ČR GAP208/11/0295; GA MŠk OC09007
    Výzkumný záměr: CEZ:AV0Z40550506; CEZ:AV0Z50520514
    Klíčová slova: cathepsin B * schistosoma * crystal structure
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 4.773, rok: 2011

    We determined three crystal structures of Schistosoma mansoni cathepsin B1 (SmCB1) in complex with peptidomimetic inhibitors. A panel of vinyl sulfone inhibitors was screened in vitro with SmCB1 and in a schistosomula assay; severity of phenotype induced in the parasite correlated with enzyme inhibition. Substrate specificity of SmCB1 was analyzed using synthetic peptides and the natural substrate, hemoglobin.
    Trvalý link: http://hdl.handle.net/11104/0200472