Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides |
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| Authors: | Di Fabio Giovanni D'Onofrio Jennifer Chiapparelli Mariateresa Hoorelbeke Bart Montesarchio Daniela Balzarini Jan De Napoli Lorenzo |
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| Institution: | 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. giovanni.difabio@unina.it |
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| Abstract: | 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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