Khandazhinskaya Anastasya L, Shirokova Elena A, Skoblov Yurii S, Victorova Lyubov S, Goryunova Ludmila Ye, Beabealashvilli Robert S, Pronyaeva Tatyana R, Fedyuk Nina V, Zolin Vladimir V, Pokrovsky Andrey G, Kukhanova Marina K
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, Russia.
J Med Chem. 2002 Mar 14;45(6):1284-91. doi: 10.1021/jm011011l.
Carbocyclic alpha, gamma-bis(nucleoside)-5,5'-triphosphonates and alpha, delta-bis(nucleoside)-5,5'-tetraphosphonates (Ap4A and Gp4G) analogues were shown to be a new type of terminating substrate of HIV reverse transcriptase. They effectively inhibited the DNA synthesis catalyzed by this enzyme in model cell-free systems, but their antiviral activity both in Rat1 fibroblast cell culture bearing MLV reverse transcriptase and in HIV-infected MT-4 cells was low. When a liposome delivery system was used, the antiviral efficacy of the compounds under study was increased.
