Inhibition of HIV-1 replication in macrophages by red blood cell-mediated delivery of a heterodinucleotide of lamivudine and tenofovir

P. Franchetti, L. Cappellacci, R. Petrelli, P. Vita, M. Grifantini, L. Rossi, F. Pierigé, S. Serafini, M. Magnani, E. Balestra, C. F. Perno

Research output: Contribution to journalArticlepeer-review

Abstract

Homo- and heterodimers of nucleoside/nucleotide analogues as reverse transcriptase inhibitors are effective on HIV-1-infected human monocyte-derived macrophages (M/M) compared to the single drugs or their combination. Since the combined treatment of lamivudine (3TC) and tenofovir ((R)PMPA) has an antiretroviral efficacy and a synergic effect respect to separate drugs, the heterodinucleotide 3TCpPMPA was synthesized. A single administration of the dimer as free drug or 3TCpPMPA-loaded RBC selectively targeted to M/M was able to almost completely protect macrophages from "de novo" infection.

Original languageEnglish
Pages (from-to)953-957
Number of pages5
JournalNucleosides, Nucleotides and Nucleic Acids
Volume26
Issue number8-9
DOIs
Publication statusPublished - Aug 2007

Keywords

  • Anti-HIV-1 activity
  • Heterodinucleotides
  • Human macrophages

ASJC Scopus subject areas

  • Genetics
  • Biochemistry

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