Number of the records: 1

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

SYSNO ASEP	0365166
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Structural Basis for Inhibition of Cathepsin B Drug Target from the Human Blood Fluke, Schistosoma mansoni
Author(s)	Jílková, Adéla (UOCHB-X)_{RID, ORCID} Řezáčová, Pavlína (UOCHB-X)_{RID, ORCID} Lepšík, Martin (UOCHB-X)_{RID, ORCID} Horn, Martin (UOCHB-X)_{RID, ORCID} Váchová, Jana (UOCHB-X) Fanfrlík, Jindřich (UOCHB-X)_{RID, ORCID} Brynda, Jiří (UOCHB-X)_{RID, ORCID} McKerrow, J. H. (US) Caffrey, C. R. (US) Mareš, Michael (UOCHB-X)_{RID, ORCID}
Number of authors	10
Source Title	Journal of Biological Chemistry. - : Elsevier - ISSN 0021-9258 Roč. 286, č. 41 (2011), s. 35770-35881
Number of pages	12 s.
Language	eng - English
Country	US - United States
Keywords	cathepsin B ; schistosoma ; crystal structure
Subject RIV	CC - Organic Chemistry
R&D Projects	GA203/09/1585 GA ČR - Czech Science Foundation (CSF)
	GAP208/11/0295 GA ČR - Czech Science Foundation (CSF)
	OC09007 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
CEZ	AV0Z40550506 - UOCHB-X (2005-2011)
	AV0Z50520514 - UMG-J (2005-2011)
UT WOS	000295927100050
DOI	10.1074/jbc.M111.271304
Annotation	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.
Workplace	Institute of Organic Chemistry and Biochemistry
Contact	asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434
Year of Publishing	2012

Number of the records: 1