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

Giovanni Di Fabio | Zendy; Jennifer D’Onofrio | Zendy; Mariateresa Chiapparelli | Zendy; Bart Hoorelbeke | Zendy; Daniela Montesarchio | Zendy; Jan Balzarini | Zendy; Lorenzo De Napoli | Zendy

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

Author(s) -

Giovanni Di Fabio,

Jennifer D’Onofrio,

Mariateresa Chiapparelli,

Bart Hoorelbeke,

Daniela Montesarchio,

Jan Balzarini,

Lorenzo De Napoli

Publication year - 2010

Publication title -

chemical communications

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.837

H-Index - 333

eISSN - 1364-548X

pISSN - 1359-7345

DOI - 10.1039/c0cc04751a

Subject(s) - phosphodiester bond , oligonucleotide , surface plasmon resonance , human immunodeficiency virus (hiv) , chemistry , g quadruplex , stereochemistry , conjugated system , selectivity , combinatorial chemistry , biochemistry , virology , biology , dna , rna , gene , nanotechnology , organic chemistry , materials science , nanoparticle , catalysis , polymer

A series of d((5')TGGGAG(3')) 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.

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