Design, synthesis, molecular modeling, and anti-HIV-1 integrase activity of a series of photoactivatable diketo acid-containing inhibitors as affinity probes (Articolo in rivista)

Type

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

Label

• Design, synthesis, molecular modeling, and anti-HIV-1 integrase activity of a series of photoactivatable diketo acid-containing inhibitors as affinity probes (Articolo in rivista) (literal)

Anno

• 2009-01-01T00:00:00+01:00 (literal)

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

• 10.1016/j.antiviral.2008.12.010 (literal)

Alternative label

• M. Sechi, F. Carta, L. Sannia, R. Dallocchio, A. Dessì, R. Al-Safi, N. Neamati (2009)
  Design, synthesis, molecular modeling, and anti-HIV-1 integrase activity of a series of photoactivatable diketo acid-containing inhibitors as affinity probes
  in Antiviral research (Print); Elsevier BV, Amsterdam (Paesi Bassi)
  (literal)

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

• M. Sechi, F. Carta, L. Sannia, R. Dallocchio, A. Dessì, R. Al-Safi, N. Neamati (literal)

Pagina inizio

• 267 (literal)

Pagina fine

• 276 (literal)

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

• 81 (literal)

Rivista

• Antiviral research (Rivista)

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

• 10 (literal)

Note

• ISI Web of Science (WOS) (literal)

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

• Istututo di Chimica Biomolecolare UOS Sassari (literal)

Titolo

• Design, synthesis, molecular modeling, and anti-HIV-1 integrase activity of a series of photoactivatable diketo acid-containing inhibitors as affinity probes (literal)

Abstract

• The diketo acid (DKA) class of HIV-1 integrase (IN) inhibitors is thought to function by chelating divalent metal ions on the enzyme catalytic site.However, differences in mutations conferring resistance to various DKA inhibitors suggest that multiple binding orientations may exist. In order to facilitate identification of DKA binding sites, a series of photoactivable analogues of two potent DKAs was prepared as novel photoaffinity probes. In cross-linking assays designed to measure disruption of substrate DNA binding, the photoprobes behaved similarly to a reference DKA inhibitor. Molecular modeling studies suggest that such photoprobes interact within the IN active site in a manner similar to that of the parent DKAs. Analogues Ia-c are novel photoaffinity ligands useful in clarifying the HIV-1 binding interactions of DKA inhibitors. (literal)

Editore

• Elsevier BV (Editore)

Prodotto di

• Istituto di chimica biomolecolare (ICB) (Istituto)
• Sintesi, caratterizzazione e studio di composti chirali e chirali non racemi di interesse biologico mediante molecole ad alta simmetria (PM.P01.011.002) (Modulo)

Autore CNR

• ALESSANDRO DESSI' (Unità di personale interno)
• ROBERTO NICO DALLOCCHIO (Persona)

Incoming links:

Autore CNR di

• ALESSANDRO DESSI' (Unità di personale interno)
• ROBERTO NICO DALLOCCHIO (Persona)

Prodotto

• Istituto di chimica biomolecolare (ICB) (Istituto)
• Sintesi, caratterizzazione e studio di composti chirali e chirali non racemi di interesse biologico mediante molecole ad alta simmetria (PM.P01.011.002) (Modulo)

Editore di

• Elsevier BV (Editore)

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

• Antiviral research (Rivista)