Journal
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
Volume 26, Issue 8-9, Pages 953-957Publisher
TAYLOR & FRANCIS INC
DOI: 10.1080/15257770701508067
Keywords
heterodinucleotides; anti-HIV-1 activity; human macrophages
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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.
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