Comparison of the effect of Carbovir, AZT, and dideoxynucleoside triphosphates on the activity of human immunodeficiency virus reverse transcriptase and selected human polymerases

E. Lucile White, William B. Parker, Lisa J. Macy, Sue C. Shaddix, George McCaleb, John A. Secrist, Robert Vince, William M. Shannon

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94 Scopus citations

Abstract

Carbocylic 2′,3′-didehydro-2′,3′-dideoxyguanosine (Carbovir; NSC 614846) is an antiretroviral agent which may be useful in the treatment of AIDS. We have synthesized the 5′-triphosphate of Carbovir and examined its ability to inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (EC 2.7.7.49) and other retroviral reverse transcriptases, as well as human DNA polymerases α, β, γ (EC 2.7.7.7) and DNA primase (EC 2.7.7.6). Carbovir triphosphate emerges as a highly selective inhibitor of reverse transcriptases with little, if any, effect on the cellular enzymes. 3′-Azido-2′,3′-dideoxythymidine (AZT) triphosphate and the two dideoxynucleoside triphosphates, ddTTP and ddGTP, inhibited HIV-1 reverse transcriptase to the same degree as Carbovir triphosphate, but were less selective in that they also inhibited DNA polymerases β and γ. We conclude that Carbovir is a highly selective antiretroviral agent.

Original languageEnglish (US)
Pages (from-to)393-398
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume161
Issue number2
DOIs
StatePublished - Jun 15 1989

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