title: Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides.
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.
authors.affiliation: 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
authors.forename: Giovanni
authors.initials: G
authors.lastname: Di Fabio
authors.forename: Jennifer
authors.initials: J
authors.lastname: D'Onofrio
authors.forename: Mariateresa
authors.initials: M
authors.lastname: Chiapparelli
authors.forename: Bart
authors.initials: B
authors.lastname: Hoorelbeke
authors.forename: Daniela
authors.initials: D
authors.lastname: Montesarchio
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.forename: Lorenzo
authors.initials: L
authors.lastname: De Napoli
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D054856:G-Quadruplexes; D006678:HIV / Q000378:metabolism; D015699:HIV Envelope Protein gp120 / Q000737:chemistry / Q000378:metabolism; D015700:HIV Envelope Protein gp41 / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D009841:Oligonucleotides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020349:Surface Plasmon Resonance
chemical_list: D019380:Anti-HIV Agents; D015699:HIV Envelope Protein gp120; D015700:HIV Envelope Protein gp41; D009841:Oligonucleotides