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.

Franchetti, P., Cappellacci, L., Petrelli, R., Vita, P., Grifantini, M., Rossi, L., et al. (2007). Inhibition of HIV-1 replication in macrophages by red blood cell-mediated delivery of a heterodinucleotide of lamivudine and tenofovir, 26(8-9), 953-957 [10.1080/15257770701508067].

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

BALESTRA, EMANUELA;PERNO, CARLO FEDERICO
2007-01-01

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.
2007
Pubblicato
Rilevanza internazionale
Articolo
Sì, ma tipo non specificato
Settore MED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICA
English
Con Impact Factor ISI
Virus Replication; Macrophages; Drug Delivery Systems; Anti-HIV Agents; Humans; Erythrocytes; Adenine; Lamivudine; Phosphonic Acids; HIV-1; Drug Design
Franchetti, P., Cappellacci, L., Petrelli, R., Vita, P., Grifantini, M., Rossi, L., et al. (2007). Inhibition of HIV-1 replication in macrophages by red blood cell-mediated delivery of a heterodinucleotide of lamivudine and tenofovir, 26(8-9), 953-957 [10.1080/15257770701508067].
Franchetti, P; Cappellacci, L; Petrelli, R; Vita, P; Grifantini, M; Rossi, L; Pierigé, F; Serafini, S; Magnani, M; Balestra, E; Perno, Cf
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/28976
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