Oligonucleotide inhibitors of HIV-1 integrase efficiently inhibit HIV-1 reverse transcriptase


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The impact of conjugates of 11-mer 2′-О-methyl oligoribonucleotides with eosin and 6-carboxy-4,7,2′,4′,5′,7′-hexachlorofluorescein on the functioning of HIV-1 reverse transcriptase (RT) was studied. These compounds were shown to inhibit the activity of RT RNase H domain. The inhibition efficiency was higher for eosin conjugates and did not depend on the oligonucleotide primary structure. The eosin conjugates were also found to block the RT polymerase activity including the mutant proteins resistant to nonnucleoside inhibitors. Since the conjugates are efficient inhibitors of HIV-1 integrase, we can assume that they belong to a new class of HIV-1 dual acting inhibitors, potentially capable of blocking several initial stages of the viral replication cycle.

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S. Korolev

Chemistry Department and Belozersky Institute of Physico-chemical Biology

编辑信件的主要联系方式.
Email: spkorolev@mail.ru
俄罗斯联邦, Moscow, 119991

T. Zatsepin

Chemistry Department and Belozersky Institute of Physico-chemical Biology

Email: spkorolev@mail.ru
俄罗斯联邦, Moscow, 119991

M. Gottikh

Chemistry Department and Belozersky Institute of Physico-chemical Biology

Email: spkorolev@mail.ru
俄罗斯联邦, Moscow, 119991

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