期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 3, 页码 960-966出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.12.051
关键词
G-quadruplex; Aptamers; Anti-HIV activity; Conjugated oligonucleotides; Solid phase synthesis
资金
- Universita degli Studi di Napoli Federico II (Finanziamento per l'Avvio di Ricerche Originali-F.A.R.O.)
- MIUR FIRB [RBFR12WB3W]
Novel conjugated G-quadruplex-forming d(TG(3)AG) oligonucleotides, linked to hydrophobic groups through phosphodiester bonds at 5'-end, have been synthesized as potential anti-HIV aptamers, via a fully automated, online phosphoramidite-based solid-phase strategy. Conjugated quadruplexes showed pronounced anti-HIV activity with some preference for HIV-1, with inhibitory activity invariably in the low micromolar range. The CD and DSC monitored thermal denaturation studies on the resulting quadruplexes, indicated the insertion of lipophilic residue at the 5'-end, conferring always improved stability to the quadruplex complex (20 < Delta Tm < 40 degrees C). The data suggest no direct functional relationship between the thermal stability and anti-HIV activity of the folded conjugated G-quartets. It would appear that the nature of the residue at 50 end of the d(TG(3)AG) quadruplexes plays an important role in the thermodynamic stabilization but a minor influence on the anti-HIV activity. Moreover, a detailed CD and DSC analyses indicate a monophasic behaviour for sequences I and V, while for ODNs (II-IV) clearly show that these quadruplex structures deviate from simple two-state melting, supporting the hypothesis that intermediate states along the dissociation pathway may exist. (C) 2014 Elsevier Ltd. All rights reserved.
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