Hairpin oligonucleotides forming G-quadruplexes: New aptamers
with anti-HIV activity

Romanucci, V; Gaglione, M; Messere, Anna; Potenza, Nicoletta; Zarrelli, A; Noppen, S; Liekens, S; Balzarini, J; Di Fabio, G.

doi:10.1016/j.ejmech.2014.10.030

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We describe the facile syntheses of new modified oligonucleotides based on d(TG3AG) that form bimolecular G-quadruplexes and possess a HEG loop as an inversion of polarity site 3'-3' or 5'-5' and aromatic residues conjugated to the 5'-end through phosphodiester bonds. The conjugated hairpin G-quadruplexes exhibited parallel orientation, high thermal stability, elevated resistance in human serum and high or moderate anti-HIV-1 activity with low cytotoxicity. Further, these molecules showed significant binding to HIV envelope glycoproteins gp120, gp41 and HSA, as revealed by SPR assays. As a result, these conjugated hairpins represent the first active anti-HIV-1 bimolecular G-quadruplexes based on the d(TG3AG) sequence.

Titolo:	Hairpin oligonucleotides forming G-quadruplexes: New aptamers with anti-HIV activity
Autori:	Romanucci V Gaglione M MESSERE, Anna POTENZA, Nicoletta Zarrelli A Noppen S Liekens S Balzarini J Di Fabio G. mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2015
Rivista:	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Abstract:	We describe the facile syntheses of new modified oligonucleotides based on d(TG3AG) that form bimolecular G-quadruplexes and possess a HEG loop as an inversion of polarity site 3'-3' or 5'-5' and aromatic residues conjugated to the 5'-end through phosphodiester bonds. The conjugated hairpin G-quadruplexes exhibited parallel orientation, high thermal stability, elevated resistance in human serum and high or moderate anti-HIV-1 activity with low cytotoxicity. Further, these molecules showed significant binding to HIV envelope glycoproteins gp120, gp41 and HSA, as revealed by SPR assays. As a result, these conjugated hairpins represent the first active anti-HIV-1 bimolecular G-quadruplexes based on the d(TG3AG) sequence.
Handle:	http://hdl.handle.net/11591/192696
Appare nelle tipologie:	1.1 Articolo in rivista

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