Autor: Hodon, J.; Sidova, V.; Urban, M.
Název práce v češtině: Studium mechanizmu účinku cytotoxických triterpenů
Název práce v angličtině: Study of the Mechanism of Action of Cytotoxic Triterpenes
Klíčová slova v češtině: cytotoxicita, triterpeny, lupan, mechanizmus účinku
Klíčová slova v angličtině:triterpenes, lupane, cytotoxicity, mechanism of action
Abstrakt česky: Byla připravena série biotinylovaných triterpenů a ty jsou v současnosti používány pro stanovení jejich mechanizmu účinku.
Abstrakt anglicky: Triterpenes are natural compounds with many interesting biological activities and every year, a number of new derivatives is either isolated from natural source or synthesized. Despite the fact that many researchers are studying this group of derivatives, their mechanisms of action often remain elusive.
In order to learn more about the mechanism of action of cytotoxic triterpenes from our research group, we are trying to find their molecular targets. In this work, a set of lupane acids was biotinylated through their 28-COOH group in order to use them in pull down assays based on biotin-streptavidin affinity purification. First, propargyl esters were prepared from free terpenic acids and biotin was modified with oligoethylene linker containing azide. Secondly, azide-alkyne Huisgen cycloaddition1 was used to connect biotinylated linker to the terpene to give final structures of general formula 1 (Fig 1). Cytotoxicity of all compounds in this study was measured. The activity of biotinylated compounds was in the similar range of the activity as their non-biotinylated parents and we can expect identification of molecular targets. The conjugates are currently being used in pull down assays evaluated by quantitative proteomics and SILAC.2 Preliminary results from pull down assays will be discussed.
Jazyk v originále: Angličtina
Publikace abstraktu: Sborník, 75/166
Forma prezentace: poster
Název konference: Advances in Organic, Bioorganic, and Pharmaceutical Chemistry „Liblice 2015“
Místo konání: Olomouc (Czech Republic)
Datum konání: November 6-8
Rok konání: 2015
Způsob financování: GACR reg. No. 15-05620S