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• W201769102 abstract "The study of new molecules able to selectively and stably interact with DNAand RNA is a field of great interest in consideration all the possible applications inmedicine. Our study is related to the biomedical applications of the final product ofPNA synthesis (the PNA itself) and the intermediate molecules obtained during thesynthetic activity. In all the chemical synthesis approach of any pharmaceuticallaboratory several molecules are produced, which are usually not considered forbiological assays and technology transfer. We screened a set of C(5) uracilderivatives monomers, that were employed during the PNA synthesis, for activity ondifferentiated functions in K562 cells. We found that the highest antiproliferative effectand erythroid induction ability was exhibited by compound 9, a thymine derivativebearing a n-octyl chain on nitrogen N(1), whereas thymine (compound 2) did notshow any effect, suggesting the importance of the linear alkil chain in N(1) position.Compound 9, furthermore, exhibits induce erythroid terminal differentiation withoutactivation of apoptotic pathway.The interest in the context on anti-tumor differentiation therapy is related to thefact that, when compared to known erythroid differentiation antitumor inducers (suchas for instance cytosine arabinoside, mithramycin, resveratrol), the lead compoundwe were able to identify is the most active agent. Therefore these molecules in ouropinion deserves further research activity in order to define its possible application,for instance in the control of proliferation/differentiation of CML primary cellsresistance to the commonly employed Imatinib (Gleevec®) therapy.As far as the final product of the synthetic strategy (a PNA recognizing miR-221 and able to be internalized in target tumor cells thanking to a linked Arg-8peptide), the results here presented allows to conclude that (a) it is internalized athigh efficiency into target tumor cells; (b) inhibits the miR-221 hybridizationavailability and (c) has important effects on biological functions regulated by miR-221(i.e. expression of the p27Kip1 mRNA/protein).These results are in our opinion of interest, considering on one hand the roleof miR-221 in cancer and, on the other hand, the role of p27Kip1.As far as miR-221, it was found to be up-regulated in several tumors; in breastcancer miR-221 is up-regulated in breast cancer cell line (such as MDA-MB-231) and in metastatic tumors. In the contest of breast cancer, it was identified p27kip1 mRNAas possible target of miR-221. The cyclin-kinase inhibitor p27kip1 is a tumorsuppressorprotein, involved in the control of cell cycle during the G0/G1 check-pointtransition: the loss or decrease of p27kip1, together with others, is one of contributorycauses of the “proliferating state” of invasive cancer, which remains in this growthphase without arrive to differentiation. It is of great interest since it was found to bedown-regulated in several type of tumors.The studies presented in this PhD Thesis teach that even intermediatesynthetic molecules deserve attention in respect to possible biological effects on cellsrelevant to human pathologies. Moreover, we have identify two reagents of possibleinterest for the development of anti-cancer protocols: N(1)-octyl-thymine for thetreatment of CML cells and Rpep-PNA-a221 for possible use in the treatment ofbreast cancer cells." @default.
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• W201769102 date "2012-03-14" @default.
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• W201769102 title "Biological activity of anti-miR-221 PeptideNucleic Acids and relative building blocks" @default.
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