The “sugar code” concept assumes the interaction of carbohydrates with inter and intra cellular components. This concept is the basis of a therapy employing carbohydrate-derived chemicals as drugs (Gabius, 2004). The “CARB” pharmacological potential is enhanced by the addition of pharmacophores and other functional groups. We proposed an idea of “functional carb-pharmacophores” (FCP) as a new approach to compose functionalized sugar derivatives that have therapeutic potential (Witczak, Poplawski, 2014) and designed the collection of FCP. For further investigation we choose sugar derivatives including thisugar and 1-4-S-thiodisacharide motifs. Our preliminary data suggest their anticancer properties, and the most sensitive was astrocytoma (HTB-14) and breast cancer (MCF-7) cell lines. The aim of this project is to determine mechanisms of anticancer activities of functional carb-pharmacophores (FCPs). Taking into account the results of our research we set the following hypotheses:  The selected FCPs kills cancer cells by activating one of the cellular death pathway.  The selected FCPs induce expression of the key genes in biological pathways activated in response to toxic drugs in cancer and normal cells  The selected FCPs induce oxidative stress in cancer cells.  The selected FCPs have inhibitory effect on proliferation cancer cells in vitro  The uptake of selected FCPs is mediated by facilitative glucose transporter proteins (GLUTs).

Evaluation of anticancer properties of thiosugars

PETRELLI, Riccardo
2015-01-01

Abstract

The “sugar code” concept assumes the interaction of carbohydrates with inter and intra cellular components. This concept is the basis of a therapy employing carbohydrate-derived chemicals as drugs (Gabius, 2004). The “CARB” pharmacological potential is enhanced by the addition of pharmacophores and other functional groups. We proposed an idea of “functional carb-pharmacophores” (FCP) as a new approach to compose functionalized sugar derivatives that have therapeutic potential (Witczak, Poplawski, 2014) and designed the collection of FCP. For further investigation we choose sugar derivatives including thisugar and 1-4-S-thiodisacharide motifs. Our preliminary data suggest their anticancer properties, and the most sensitive was astrocytoma (HTB-14) and breast cancer (MCF-7) cell lines. The aim of this project is to determine mechanisms of anticancer activities of functional carb-pharmacophores (FCPs). Taking into account the results of our research we set the following hypotheses:  The selected FCPs kills cancer cells by activating one of the cellular death pathway.  The selected FCPs induce expression of the key genes in biological pathways activated in response to toxic drugs in cancer and normal cells  The selected FCPs induce oxidative stress in cancer cells.  The selected FCPs have inhibitory effect on proliferation cancer cells in vitro  The uptake of selected FCPs is mediated by facilitative glucose transporter proteins (GLUTs).
2015
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/381181
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