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Organoruthenium glycomimetics as selective galectin-1 inhibitors
Hamala, Vojtěch
The prepared organoruthenium glycomimetics demonstrated sin gle unit nanomolar affinity to Gal-1 and over four orders of magnitude\nhigher selectivity to Gal-1 in comparison to Gal-3. The organoruthe nium galectin inhibitors were found to be nontoxic to both cancer and\nnoncancerous cell lines. Selected complexes showed an in vitro an timigratory effect against invasive cancer cell lines MDA-MB-231 and\nSK-OV-3.
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Hybrid organometallic galectin inhibitors
Hamala, Vojtěch
Galectins are lectin-type proteins defined by their sequence homology and the ability to bind β-galactosides. Human galectin-1 (Gal-1) and galectin-3 (Gal-3) are involved in tumor progression. Elevated Gal-1 levels are reported for many tumor tissues and Gal-1 contributes to tumor progression including cell migration and tumor immune escape.\nGal-3 is characteristically overexpressed in many cancers and an elevated Gal-3 level is associated with increased invasiveness, metastatic spreading, immunosuppression and angiogenesis. Galectins are also implicated in progression of serious diseases other than cancer e.g., cardiovascular ones, diabetes mellitus, fibrosis, and others. These\nproperties make galectins promising therapeutic targets.\n
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Synthesis and Cytotoxicity of Fluorinated Amino Saccharides.
Hamala, Vojtěch
This work presents the synthesis of acetyl, propionyl, and butyrylesters of monofluorinated, difluorinated, and trifluorinated analogues\nof N-acetyl-d-glucosamine and N-acetyl-d-galactosamine, and theircytotoxicity expressed as IC50 values against the MDA-MB-231 cancer\ncell line (triple-negative breast cancer) along with their IC50 valuesagainst the HEK-293 non-cancerous cell line.
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