Issue 8, 2011
From the journal:

Chemical Communications

Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides†‡

Giovanni Di Fabio,*a   Jennifer D'Onofrio,a   Mariateresa Chiapparelli,a   Bart Hoorelbeke,b   Daniela Montesarchio,a   Jan Balzarinib  and  Lorenzo De Napolia  

* Corresponding authors

a Dipartimento di Chimica Organica e Biochimica, Università degli Studi di Napoli “Federico II”, Complesso Universitario di Monte S. Angelo, via Cintia, 4, I-80126 Napoli, Italy
E-mail: giovanni.difabio@unina.it
Fax: +39 081-674393
Tel: +39 081-674001

b Rega Institute for Medical Research, Katholieke Universiteit Leuven, 10 Minderbroedersstraat, B-3000 Leuven, Belgium

Abstract

A series of d(5′TGGGAG3′) sequences, 5′-conjugated with a variety of aromatic groups through phosphodiester linkages, were synthesized, showing CD spectra diagnostic of parallel-stranded, tetramolecular G-quadruplex structures. When tested for anti-HIV-1 and HIV-2 activity, potent inhibition of HIV-1 infection in CEM cell cultures was found, associated with high selectivity index values. Surface Plasmon Resonance assays revealed specific binding to HIV-1 gp120 and gp41.

Graphical abstract: Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides

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Article information

DOI
https://doi.org/10.1039/C0CC04751A
Article type
Communication
Submitted
02 Nov 2010
Accepted
23 Nov 2010
First published
16 Dec 2010

Chem. Commun., 2011,47, 2363-2365

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Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides

G. Di Fabio, J. D'Onofrio, M. Chiapparelli, B. Hoorelbeke, D. Montesarchio, J. Balzarini and L. De Napoli, Chem. Commun., 2011, 47, 2363 DOI: 10.1039/C0CC04751A

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