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Enzyme kinetic evaluation of several potential inhibitors of certain human cysteine and serine proteases
Hympánová, Michaela ; Konečná, Klára (advisor) ; Janďourek, Ondřej (referee)
IN ENGLISH Charles University Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Supervisors: prof. Dr. Michael Gütschow RNDr. Klára Konečná, Ph.D. Candidate: Michaela Hympánová Title of the diploma thesis: Enzyme kinetic evaluation of several potential inhibitors of certain human cysteine and serine proteases Background Cysteine and serine proteases are enzymes involved in many physiological processes. The imbalance between them and their endogenous inhibitors is associated with various diseases such as cancer and osteoporosis. Synthetic inactivators could be useful in the treatment of these enzyme-mediated pathological conditions. Therefore, there are ongoing attempts to develop low-molecular weight inactivators for therapeutically relevant cysteine and serine proteases. In the course of this thesis, compounds synthesized in prof. Gütschow's group were investigated as potential inhibitors of selected human proteases. They belong to imidazole compounds derived from N-protected cyclohexylalanine, 2-phenyl-7,8-dihydroimidazo[1,2- a]pyrazin-6(5H)-one derivatives, ,-unsaturated peptidomimetic compounds, carbamates, an N,N-dibenzylcrotonamide derivatives and peptoides. Aims This diploma thesis has been focused on the evaluation of new potential inhibitors against...
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Virulence factors of Entamoeba histolytica
Novotná, Monika ; Tachezy, Jan (advisor) ; Tůmová, Pavla (referee)
The parasitic protist Entamoeba histolytica causes intestinal disease called amoebiasis (amoebic dysentery), which is one of the most significant diseases worldwide, mainly in developing countries. The goal of this bachelor thesis is to summarize current knowledge about virulence factors of E. histolytica. It is primarly focused on adhesive lectin Gal/GalNAc, cysteine proteases, phagocytosis of apoptotic cells, amoebapore forming pores in the membranes of the target cells and trogocytosis. Keywords: virulence factors, Entamoeba histolytica, parasite, protist, amoebiasis, lectin Gal/GalNAc, cysteine proteinase, phagocytosis, trogocytosis, amoebapore
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Detekce a kvantifikace inhibitorů proteáz v klíštěti \kur{Ixodes ricinus} pomocí monoklonálních protilátek
VANÍČKOVÁ, Martina
Inhibitors of proteases in tick saliva play an important role during tick feeding. Tick saliva contains a wide range of bioactive components which are able to modulate host imunity. Therefore, ticks are able to feed for a long time and transfer tick-borne diseases pathogens. The risk of transfer can be significantly reduced by deactivation of theese protease inhibitors. In this study I made monoclonal antibodies for detection and quantification of two serine protease inhibitors in tick saliva and other tick-body parts.
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Enzyme kinetic evaluation of several potential inhibitors of certain human cysteine and serine proteases
Hympánová, Michaela ; Konečná, Klára (advisor) ; Janďourek, Ondřej (referee)
IN ENGLISH Charles University Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Supervisors: prof. Dr. Michael Gütschow RNDr. Klára Konečná, Ph.D. Candidate: Michaela Hympánová Title of the diploma thesis: Enzyme kinetic evaluation of several potential inhibitors of certain human cysteine and serine proteases Background Cysteine and serine proteases are enzymes involved in many physiological processes. The imbalance between them and their endogenous inhibitors is associated with various diseases such as cancer and osteoporosis. Synthetic inactivators could be useful in the treatment of these enzyme-mediated pathological conditions. Therefore, there are ongoing attempts to develop low-molecular weight inactivators for therapeutically relevant cysteine and serine proteases. In the course of this thesis, compounds synthesized in prof. Gütschow's group were investigated as potential inhibitors of selected human proteases. They belong to imidazole compounds derived from N-protected cyclohexylalanine, 2-phenyl-7,8-dihydroimidazo[1,2- a]pyrazin-6(5H)-one derivatives, ,-unsaturated peptidomimetic compounds, carbamates, an N,N-dibenzylcrotonamide derivatives and peptoides. Aims This diploma thesis has been focused on the evaluation of new potential inhibitors against...
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Factors regulating the expression and activity of digestive enzymes in the tick \kur{Ixodes ricinus}
KONVIČKOVÁ, Jitka
The intracellular proteolysis of ingested meal plays an essential role in tick development. The thesis focuses on the factors influencing the expressions and activities of digestive enzymes in Ixodes ricinus females during the feeding and post-feeding period. We have revealed the effect of fertilization on blood feeding and digestion. The females cannot reach the rapid engorgement phase without being fertilized. The rate of mated females in the nature proved the presumption that mating can occur even off the host. Implementation of in vitro feeding technique further extended our current knowledge about tick digestive apparatus. Adult females were fed on hemoglobin-rich and hemoglobin-poor diet and the mRNA expression levels of digestive proteases were determined. In line with obtained data, we assumed that albuminolysis is conducted by the same or similar pathway as hemoglobinolysis. The gene silencing method and protein immuno-detection were used to unequivocally identify the isoforms of 'early expressed' IrCL1 and 'late expressed' IrCL3 isoform of cathepsin L.
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