Enhancement of Anti-HIV-1 Activity by Hot Spot Evolution of RANTES-Derived Peptides (Articolo in rivista)

Type
Label
  • Enhancement of Anti-HIV-1 Activity by Hot Spot Evolution of RANTES-Derived Peptides (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.chembiol.2012.10.007 (literal)
Alternative label
  • Secchi, Massimiliano; Longhi, Renato; Vassena, Lia; Sironi, Francesca; Grzesiek, Stephan; Lusso, Paolo; Vangelista, Luca (2012)
    Enhancement of Anti-HIV-1 Activity by Hot Spot Evolution of RANTES-Derived Peptides
    in Chemistry & biology (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Secchi, Massimiliano; Longhi, Renato; Vassena, Lia; Sironi, Francesca; Grzesiek, Stephan; Lusso, Paolo; Vangelista, Luca (literal)
Pagina inizio
  • 1579 (literal)
Pagina fine
  • 1588 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 19 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 10 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 12 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Vita-Salute San Raffaele University; Consiglio Nazionale delle Ricerche (CNR); University of Basel; University of Cagliari (literal)
Titolo
  • Enhancement of Anti-HIV-1 Activity by Hot Spot Evolution of RANTES-Derived Peptides (literal)
Abstract
  • CCR5, the major HIV-1 coreceptor, is a primary target for HIV-1 entry inhibition strategies. CCL5/RANTES, a natural CCR5 ligand, is one of the most potent HIV-1 entry inhibitors and, therefore, an ideal candidate to derive HIV-1 blockers. Peptides spanning the RANTES N-loop/beta 1-strand region act as specific CCR5 antagonists, with their hydrophobic N- and C termini playing a crucial role in virus blockade. Here, hydrophobic surfaces were enhanced by tryptophan substitution of aromatic residues, highlighting position 27 as a critical hot spot for HIV-1 blockade. In a further molecular evolution step, C-terminal engraftment of RANTES 40' loop produced a peptide with the highest solubility and anti-HIV-1 activity. These modified peptides represent leads for the development of effective HIV-1 inhibitors and microbicides. (literal)
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