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  • "The function of capthepsin is controlled on several levels and failure at any level can lead to a serious pathological state. The aim of the project is to investigate selected cysteine and aspartic lysosomal proteinases, namely cathepsin C and cathepsin D, on different structural levels (primary structure, posttranslational modifications, tertiary and quaternary structure) as the basis for explanation of their activity, specificity, and interaction with inhibitors. Inhibitor topic is focused on characterization of two categories of inhibitors"" (i) novel synthetic inhibitors of peptide type, (ii) natural inhibitors of protein character. The research includes determination of their 3D structure (by X-ray crystallogrphy) and description of interaction mode with cognate proteinases. PThe project will provide information for a better understanding of cathepsins action, inhibitory regulation and intracellular targeting, as well as the role of cathepsins in human pathogenesis." (en)
  • "Funkce kathepsinů je kontrolována na několika úrovních a porucha regulace kterékoli z nich má za následek vznik patologických stavů. Cílem projektu je analysa vybraných cysteinových a aspartátových proteinas, konkrétně kathepsinu C a kathepsinu D, na několika strukturních rovinách (primární struktura posttranslační modifikace, terciální a kvartérní struktura) jako strukturní základ pro vysvětlení jejich aktivity, specificity a interakce s inhibitory. Studium inhibitorů se soustředí na dvě kategorie inhibitorů "" (i) nové syntetické inhibitory peptidového typu, (ii) přirozené inhibitory proteinového charakteru. Určena bude jejich prostorová struktura (X-paprskovou krystalografií) a mechanismus interakce s lysosomálními proteinasami. Projket poskytne informace o působení kathepsinů, jejich inhibiční regulaci a nitrobuněčném transportu a také o roli kathepsinů v humánní patogenesi." (cs)
Title
  • Structural and functional characterization of cathepsins and their inhibitors (en)
  • Strukturní a funkční charakterizace kathepsinů a jejich inhibitorů (cs)
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  • cathepsin; structure-function; inhibitor; (en)
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