" protein" . . "Schistosomiasis, caused by blood fluke (Schistosoma), is major global health problem affecting 200 million people. Viability of the parasite worms is dependent on hemoglobinolysis maintained by gut-associated proteolytic enzymes. These digestive enzymes represent new target for suppression of blood fluke metabolism. The project focuses on design and synthesis of specific inhibitors of three schistosomal peptidases. The inhibitors will be designed based on (a) the functional scaffolds discovered by the applicant, and (b) the strategy utilizing combinatorial chemistry and rational design with the use of molecular (homology and crystallographic) models. Screening of the synthesized inhibitors will be performed with the target peptidases prepared by microseparation from the parasites and by expression as recombinant enzymes. The project will provide novel small-molecule structures as leads for the development of antischistosomal chemotherapeutics."@en . "Parasite-targeted peptidase inhibitors as a tool for schistosomiasis therapy."@en . . . . . "GA203/09/1585" . "V\u00FDvoj inhibitor\u016F proteas pro l\u00E9\u010Dbu schistosom\u00F3zy." . . " fluke" . "The project provided new data concerning of structure/function relationships of peptidases of parasite S.mansoni. Selective inhibitors of peptidases were obtained. The project was focused on cathepsine B1,C and D. 3 papers were published, 2 more are prepared. The funding was according the scheduled plan. Aims of the project were fulfilled. It can be stated that grant proposal was accomplished."@en . "2014-01-30+01:00"^^ . "2012-03-30+02:00"^^ . . " Schistosomiasis" . . " structure" . . "http://www.isvav.cz/projectDetail.do?rowId=GA203/09/1585"^^ . . "Projekt p\u0159inesl informace o vztahu struktury/funkce peptidas parazita Schistosoma mansoni. Byly z\u00EDsk\u00E1ny nov\u00E9 selektivn\u00ED inhibitory peptidas. Projekt se zam\u011B\u0159il na katepsiny B1,C a D. Napln\u011Bn\u00ED c\u00EDl\u016F projektu je dolo\u017Eeno 3 publikovan\u00FDm pracemi, 2 se p\u0159ipravuj\u00ED. Z\u00E1m\u011Bry deklarovan\u00E9 v zad\u00E1n\u00ED projektu byly napln\u011Bny. \u010Cerp\u00E1n\u00ED finan\u010Dn\u00EDch prost\u0159edk\u016F bylo dle zad\u00E1n\u00ED. \u0158e\u0161en\u00ED projektu lze hodnotit jako spln\u011Bn\u00E9."@cs . . . . "2012-12-31+01:00"^^ . . . "5"^^ . "5"^^ . "0"^^ . . "1"^^ . "blood; fluke; peptidase; inhibitors; protein; structure; Schistosomiasis; chemotherapy"@en . . . "Schistosom\u00F3za postihuj\u00EDc\u00ED 200 mili\u00F3n\u016F lid\u00ED pat\u0159\u00ED mezi nejz\u00E1va\u017En\u011Bj\u0161\u00ED parazit\u00E1rn\u00ED onemocn\u011Bn\u00ED \u010Dlov\u011Bka. P\u016Fvodcem infekce je krevni\u010Dka rodu Schistosoma \u017Eiv\u00EDc\u00ED se krv\u00ED hostitele. \u017Divotaschopnost parazita z\u00E1vis\u00ED na degradaci p\u0159ijat\u00E9ho hemoglobinu pomoc\u00ED tr\u00E1vic\u00EDch peptidas krevni\u010Dky. Tyto peptidasy p\u0159edstavuj\u00ED nov\u00FD c\u00EDl pro supresi metabolismu krevni\u010Dky. Projekt se zab\u00FDv\u00E1 v\u00FDvojem a synt\u00E9zou specifick\u00FDch inhibitor\u016F t\u0159\u00ED schistosom\u00E1ln\u00EDch peptidas. Inhibitory budou navr\u017Eeny (a) podle funk\u010Dn\u00EDch templ\u00E1t\u016F objeven\u00FDch \u0159e\u0161itelem a (b) pomoc\u00ED strategie spojuj\u00EDc\u00ED kombinatorn\u00ED chemii a racion\u00E1ln\u00ED design s vyu\u017Eit\u00EDm molekul\u00E1rn\u00EDch (homologn\u00EDch a krystalografick\u00FDch) model\u016F. Syntetizovan\u00E9 inhibitory budou testov\u00E1ny na c\u00EDlov\u00FDch peptidasach p\u0159ipraven\u00FDch mikroizolac\u00ED z parazit\u016F nebo rekombinantn\u00ED expres\u00ED. Projekt p\u0159inese nov\u00E9 inhibi\u010Dn\u00ED struktury pro v\u00FDvoj antischistosom\u00E1ln\u00EDch chemoterapeutik." . "0"^^ . "blood" . " inhibitors" . " peptidase" . "2009-01-01+01:00"^^ . . .