Romanucci, Valeria (2015) G-quadruplexes: design, synthesis and characterization of new modified ODNs and natural ligands. [Tesi di dottorato]

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Item Type: Tesi di dottorato
Lingua: English
Title: G-quadruplexes: design, synthesis and characterization of new modified ODNs and natural ligands.
Creators:
CreatorsEmail
Romanucci, Valeriavaleria.romanucci@unina.it
Date: 30 March 2015
Number of Pages: 195
Institution: Università degli Studi di Napoli Federico II
Department: Scienze Chimiche
Scuola di dottorato: Scienze chimiche
Dottorato: Scienze chimiche
Ciclo di dottorato: 27
Coordinatore del Corso di dottorato:
nomeemail
Paduano, Luigiluigi.paduano@unina.it
Tutor:
nomeemail
Di Fabio, GiovanniUNSPECIFIED
Date: 30 March 2015
Number of Pages: 195
Uncontrolled Keywords: 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
Date Deposited: 09 Apr 2015 09:16
Last Modified: 08 Jun 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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