Synthesis, biophysical characterization and anti-HIV activity of d(TG(3)AG) Quadruplexes bearing hydrophobic tails at the 5 '-end (Articolo in rivista)

Type

• Prodotto della ricerca (Classe)
• Articolo in rivista (Classe)

Label

• Synthesis, biophysical characterization and anti-HIV activity of d(TG(3)AG) Quadruplexes bearing hydrophobic tails at the 5 '-end (Articolo in rivista) (literal)

Anno

• 2014-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1016/j.bmc.2013.12.051 (literal)

Alternative label

• Romanucci, Valeria; Milardi, Danilo; Campagna, Tiziana; Gaglione, Maria; Messere, Anna; D'Urso, Alessandro; Crisafi, Emanuela; La Rosa, Carmelo; Zarrelli, Armando; Balzarini, Jan; Di Fabio, Giovanni (2014)
  Synthesis, biophysical characterization and anti-HIV activity of d(TG(3)AG) Quadruplexes bearing hydrophobic tails at the 5 '-end
  in Bioorganic & medicinal chemistry (Print)
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Romanucci, Valeria; Milardi, Danilo; Campagna, Tiziana; Gaglione, Maria; Messere, Anna; D'Urso, Alessandro; Crisafi, Emanuela; La Rosa, Carmelo; Zarrelli, Armando; Balzarini, Jan; Di Fabio, Giovanni (literal)

Pagina inizio

• 960 (literal)

Pagina fine

• 966 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 22 (literal)

Rivista

• Bioorganic & medicinal chemistry (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali

• 7 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

• 3 (literal)

Note

• ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• University of Naples Federico II; Consiglio Nazionale delle Ricerche (CNR); Seconda Universita degli Studi di Napoli; University of Catania; KU Leuven (literal)

Titolo

• Synthesis, biophysical characterization and anti-HIV activity of d(TG(3)AG) Quadruplexes bearing hydrophobic tails at the 5 '-end (literal)

Abstract

• Novel conjugated G-quadruplex-forming d(TG(3)AG) oligonucleotides, linked to hydrophobic groups through phosphodiester bonds at 5'-end, have been synthesized as potential anti-HIV aptamers, via a fully automated, online phosphoramidite-based solid-phase strategy. Conjugated quadruplexes showed pronounced anti-HIV activity with some preference for HIV-1, with inhibitory activity invariably in the low micromolar range. The CD and DSC monitored thermal denaturation studies on the resulting quadruplexes, indicated the insertion of lipophilic residue at the 5'-end, conferring always improved stability to the quadruplex complex (20 < Delta Tm < 40 degrees C). The data suggest no direct functional relationship between the thermal stability and anti-HIV activity of the folded conjugated G-quartets. It would appear that the nature of the residue at 50 end of the d(TG(3)AG) quadruplexes plays an important role in the thermodynamic stabilization but a minor influence on the anti-HIV activity. Moreover, a detailed CD and DSC analyses indicate a monophasic behaviour for sequences I and V, while for ODNs (II-IV) clearly show that these quadruplex structures deviate from simple two-state melting, supporting the hypothesis that intermediate states along the dissociation pathway may exist. (C) 2014 Elsevier Ltd. All rights reserved. (literal)

Prodotto di

• Progettazione e sintesi di nuovi composti bioattivi e loro veicolazione sito specifica. (PM.P01.003.002) (Modulo)
• Institute of biostructure and bioimaging (IBB) (Istituto)

Autore CNR

• DANILO MILARDI (Persona)

Insieme di parole chiave

• Keywords of "Synthesis, biophysical characterization and anti-HIV activity of d(TG(3)AG) Quadruplexes bearing hydrophobic tails at the 5 '-end" (Insieme di parole chiave)

Incoming links:

Autore CNR di

• DANILO MILARDI (Persona)

Prodotto

• Institute of biostructure and bioimaging (IBB) (Istituto)
• Progettazione e sintesi di nuovi composti bioattivi e loro veicolazione sito specifica. (PM.P01.003.002) (Modulo)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• Bioorganic & medicinal chemistry (Rivista)

Insieme di parole chiave di

• Keywords of "Synthesis, biophysical characterization and anti-HIV activity of d(TG(3)AG) Quadruplexes bearing hydrophobic tails at the 5 '-end" (Insieme di parole chiave)