New anti-HIV aptamers based on tetra-end-linked DNA G-quadruplexes: effect of the base sequence on anti-HIV activity

Valentina D'Atri; Giorgia Oliviero; Jussara Amato; Nicola Borbone; Stefano D'Errico; Luciano Mayol; Vincenzo Piccialli; Shozeb Haider; Bart Hoorelbeke; Jan Balzarini; Gennaro Piccialli

doi:10.1039/C2CC34399A

New anti-HIV aptamers based on tetra-end-linked DNA G-quadruplexes: effect of the base sequence on anti-HIV activity†

Valentina D'Atri,^a Giorgia Oliviero,^a Jussara Amato,^a Nicola Borbone,*^a Stefano D'Errico,^a Luciano Mayol,^a Vincenzo Piccialli,^b Shozeb Haider,^c Bart Hoorelbeke,^d Jan Balzarini^d and Gennaro Piccialli^a

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* Corresponding authors

^a Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli Federico II, Via D. Montesano 49, I-80131 Napoli, Italy
E-mail: Nicola.borbone@unina.it

^b Dipartimento di Chimica, Università degli Studi di Napoli Federico II, Via Cynthia 4, I-80126 Napoli, Italy

^c Centre for Cancer Research and Cell Biology, Queen's University of Belfast, 97 Lisburn Road, Belfast, UK

^d Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium

Abstract

This communication reports on the synthesis and biophysical, biological and SAR studies of a small library of new anti-HIV aptamers based on the tetra-end-linked G-quadruplex structure. The new aptamers showed EC₅₀ values against HIV-1 in the range of 0.04–0.15 μM as well as affinities for the HIV-1 gp120 envelope in the same order of magnitude.

Chemical Communications

New anti-HIV aptamers based on tetra-end-linked DNA G-quadruplexes: effect of the base sequence on anti-HIV activity†

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