"Horn, Martin" . . "5"^^ . . "RIV/61388963:_____/11:00360455" . "Caffrey, C. R." . "ACS Chemical Biology" . . . . "J\u00EDlkov\u00E1, Ad\u00E9la" . . "000291896400011" . "Mapping the Pro-Peptide of the Schistosoma mansoni Cathepsin B1 Drug Target: Modulation of Inhibition by Heparin and Design of Mimetic Inhibitors" . . . "210640" . "Mare\u0161, Michael" . "Schistosoma mansoni; cathepsin B; propeptide"@en . "I, P(GA203/09/1585), P(IAA400550705), P(KJB400550516), Z(AV0Z40550506)" . . . . "10.1021/cb100411v" . . "Mapping the Pro-Peptide of the Schistosoma mansoni Cathepsin B1 Drug Target: Modulation of Inhibition by Heparin and Design of Mimetic Inhibitors"@en . "Mare\u0161ov\u00E1, Lucie" . . . "9"^^ . . . "[FE09680467A8]" . . . "US - Spojen\u00E9 st\u00E1ty americk\u00E9" . "6" . . . "Vondr\u00E1\u0161ek, Ji\u0159\u00ED" . "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." . "Mapping the Pro-Peptide of the Schistosoma mansoni Cathepsin B1 Drug Target: Modulation of Inhibition by Heparin and Design of Mimetic Inhibitors" . . . . . "RIV/61388963:_____/11:00360455!RIV12-AV0-61388963" . "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."@en . "1554-8929" . "6"^^ . "Mapping the Pro-Peptide of the Schistosoma mansoni Cathepsin B1 Drug Target: Modulation of Inhibition by Heparin and Design of Mimetic Inhibitors"@en . . "6" .