title: Screening Platform toward New Anti-HIV Aptamers Set on Molecular Docking and Fluorescence Quenching Techniques.
abstract: By using a new rapid screening platform set on molecular docking simulations and fluorescence quenching techniques, three new anti-HIV aptamers targeting the viral surface glycoprotein 120 (gp120) were selected, synthesized, and assayed. The use of the short synthetic fluorescent peptide V35-Fluo mimicking the V3 loop of gp120, as the molecular target for fluorescence-quenching binding affinity studies, allowed one to measure the binding affinities of the new aptamers for the HIV-1 gp120 without the need to obtain and purify the full recombinant gp120 protein. The almost perfect correspondence between the calculated Kd and the experimental EC50 on HIV-infected cells confirmed the reliability of the platform as an alternative to the existing methods for aptamer selection and measuring of aptamer-protein equilibria.
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Giorgia
authors.initials: G
authors.lastname: Oliviero
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Mariano
authors.initials: M
authors.lastname: Stornaiuolo
authors.affiliation: University of Bordeaux , IECB, ARNA laboratory, Pessac, 33600, France.|INSERM , U869, ARNA laboratory, Bordeaux, 33000, France.
authors.forename: Valentina
authors.initials: V
authors.lastname: D'Atri
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Fabrizia
authors.initials: F
authors.lastname: Nici
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Ali Munaim
authors.initials: AM
authors.lastname: Yousif
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: D'Errico
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.|CNR , Institute of Protein Biochemistry, Napoli, 80131, Italy.
authors.forename: Gennaro
authors.initials: G
authors.lastname: Piccialli
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Luciano
authors.initials: L
authors.lastname: Mayol
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Luciana
authors.initials: L
authors.lastname: Marinelli
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Grieco
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Alfonso
authors.initials: A
authors.lastname: Carotenuto
authors.affiliation: KU Leuven , Rega Institute for Medical Research, Leuven, 3000, Belgium.
authors.forename: Sam
authors.initials: S
authors.lastname: Noppen
authors.affiliation: KU Leuven , Rega Institute for Medical Research, Leuven, 3000, Belgium.
authors.forename: Sandra
authors.initials: S
authors.lastname: Liekens
authors.affiliation: KU Leuven , Rega Institute for Medical Research, Leuven, 3000, Belgium.
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.affiliation: University of Naples Federico II , Department of Pharmacy, Napoli, 80131, Italy.
authors.forename: Nicola
authors.initials: N
authors.lastname: Borbone
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D052157:Aptamers, Nucleotide / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D005453:Fluorescence; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry; D006678:HIV / Q000187:drug effects / Q000378:metabolism; D015699:HIV Envelope Protein gp120 / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D062105:Molecular Docking Simulation; D015203:Reproducibility of Results; D013050:Spectrometry, Fluorescence; D013816:Thermodynamics
chemical_list: D019380:Anti-HIV Agents; D052157:Aptamers, Nucleotide; D005456:Fluorescent Dyes; D015699:HIV Envelope Protein gp120