Romanucci, Valeria (2015) G-quadruplexes: design, synthesis and characterization of new modified ODNs and natural ligands. [Tesi di dottorato]
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| Tipologia del documento: | Tesi di dottorato |
|---|---|
| Lingua: | English |
| Titolo: | G-quadruplexes: design, synthesis and characterization of new modified ODNs and natural ligands. |
| Autori: | Autore Email Romanucci, Valeria valeria.romanucci@unina.it |
| Data: | 30 Marzo 2015 |
| Numero di pagine: | 195 |
| Istituzione: | Università degli Studi di Napoli Federico II |
| Dipartimento: | Scienze Chimiche |
| Scuola di dottorato: | Scienze chimiche |
| Dottorato: | Scienze chimiche |
| Ciclo di dottorato: | 27 |
| Coordinatore del Corso di dottorato: | nome email Paduano, Luigi luigi.paduano@unina.it |
| Tutor: | nome email Di Fabio, Giovanni [non definito] |
| Data: | 30 Marzo 2015 |
| Numero di pagine: | 195 |
| Parole chiave: | G-quadruplex;anti-HIV;aptamer;natural products;silibinin;telomerase activity;modified oligonucleotides;G-quadruplex-ligands |
| Settori scientifico-disciplinari del MIUR: | Area 03 - Scienze chimiche > CHIM/06 - Chimica organica |
| Aree tematiche (7° programma Quadro): | SALUTE e TUTELA DEL CONSUMATORE > Biotecnologie, strumenti e tecnologie generiche per la salute umana |
| Depositato il: | 09 Apr 2015 09:16 |
| Ultima modifica: | 08 Giu 2018 01:00 |
| URI: | http://www.fedoa.unina.it/id/eprint/10116 |
| DOI: | 10.6093/UNINA/FEDOA/10116 |
Abstract
PhD project is focused on the synthesis and biophysically and biologically characterization of a new mini-library of d(TGGGAG) oligomers as potential anti-HIV. It has been developed an efficient procedure to synthesize modified d(TGGGAG) oligomers carrying hydrophobic and aromatic groups at the 5'-end by a phosphodiester bond. In addition, aiming at improving the kinetic of G-quadruplex formation using d(TGGGAG) as a lead sequence, it have been synthesized bimolecular G-quadruplexes based on d(TGGGAG) sequence containing a HEG loop as a 3'-3' or 5'-5' inversion of polarity site. Kinetic studies of G-quadruplex formation based on the most active 5'-end modified d(TGGGAG) sequences are carried out using ESI-Mass Spectrometry. The interest in G-quadruplex structures has greatly expanded for their existence in vivo in several important oncogenes and in human telomeres. Many antitumor strategies have been developed on the inhibition of telomerase activity through the use of specific ligands. In this frame, it has been analysed the potentiality of a natural compound, namely silibinin. It has been performed an efficient HPLC preparative method to obtain the pure form of silibinin (silybin A and B), and it has been developed a base-catalyzed oxidation of silybin A and B by microwave (MW), which leads to biologically interesting product: the 2,3-dehydrosilybin A and B.
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