Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.

The sensitivities of reverse transcriptases (RTs) from feline immunodeficiency virus (FIV) and human immunodeficiency virus type 1 (HIV) were directly compared. The two enzymes had similar sensitivities to three analogs of dTTP, namely, 3'-azido-3'-deoxythymidine 5'-triphosphate, 2�...

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Main Authors: North, T W, Cronn, R C, Remington, K M, Tandberg, R T
Formato: Artigo
Idioma:en
Publicado em: 1990
Assuntos:
Research Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC171861/
https://ncbi.nlm.nih.gov/pubmed/1699491
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spelling pubmed-1718612003-12-01 Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses. North, T W Cronn, R C Remington, K M Tandberg, R T Antimicrob Agents Chemother Research Article The sensitivities of reverse transcriptases (RTs) from feline immunodeficiency virus (FIV) and human immunodeficiency virus type 1 (HIV) were directly compared. The two enzymes had similar sensitivities to three analogs of dTTP, namely, 3'-azido-3'-deoxythymidine 5'-triphosphate, 2',3'-dideoxythymidine 5'-triphosphate, and 2',3'-dideoxy-2',3'-didehydrothymidine 5'-triphosphate. Each of these analogs demonstrated competitive inhibition of both enzymes. Ki values for inhibition of FIV RT by these three inhibitors were 3.3, 6.7, and 1.8 nM, respectively; Ki values for inhibition of the HIV enzyme were 6.5, 5.9, and 8.3 nM, respectively. Ratios of the Ki for the inhibitor to the Km for the substrate were also determined for each inhibitor, and no differences between the two enzymes greater than threefold were observed. Inhibition constants for 3'-amino-3'-deoxythymidine 5'-triphosphate and 3'-fluoro-3'-deoxythymidine 5'-triphosphate were determined for FIV RT, and these were similar to published values for HIV RT. The activities of three dideoxynucleoside 5'-triphosphates against FIV RT were determined; ddGTP was slightly more potent than ddTTP, whereas both were much more effective than ddCTP. The activity of a noncompetitive inhibitor, phosphonoformate, was also examined with the FIV enzyme; it was much more active with poly(rA)-oligo(dT) as the template-primer than with poly(rC)-oligo(dG) or poly(rI)-oligo(dC). 1990-08 /pmc/articles/PMC171861/ /pubmed/1699491 Text en
institution US National Library of Medicine
collection PubMed Central
language en
format Article
topic Research Article
spellingShingle Research Article
North, T W
Cronn, R C
Remington, K M
Tandberg, R T
Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
description The sensitivities of reverse transcriptases (RTs) from feline immunodeficiency virus (FIV) and human immunodeficiency virus type 1 (HIV) were directly compared. The two enzymes had similar sensitivities to three analogs of dTTP, namely, 3'-azido-3'-deoxythymidine 5'-triphosphate, 2',3'-dideoxythymidine 5'-triphosphate, and 2',3'-dideoxy-2',3'-didehydrothymidine 5'-triphosphate. Each of these analogs demonstrated competitive inhibition of both enzymes. Ki values for inhibition of FIV RT by these three inhibitors were 3.3, 6.7, and 1.8 nM, respectively; Ki values for inhibition of the HIV enzyme were 6.5, 5.9, and 8.3 nM, respectively. Ratios of the Ki for the inhibitor to the Km for the substrate were also determined for each inhibitor, and no differences between the two enzymes greater than threefold were observed. Inhibition constants for 3'-amino-3'-deoxythymidine 5'-triphosphate and 3'-fluoro-3'-deoxythymidine 5'-triphosphate were determined for FIV RT, and these were similar to published values for HIV RT. The activities of three dideoxynucleoside 5'-triphosphates against FIV RT were determined; ddGTP was slightly more potent than ddTTP, whereas both were much more effective than ddCTP. The activity of a noncompetitive inhibitor, phosphonoformate, was also examined with the FIV enzyme; it was much more active with poly(rA)-oligo(dT) as the template-primer than with poly(rC)-oligo(dG) or poly(rI)-oligo(dC).
author North, T W
Cronn, R C
Remington, K M
Tandberg, R T
author_facet North, T W
Cronn, R C
Remington, K M
Tandberg, R T
author_sort North, T W
title Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
title_short Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
title_full Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
title_fullStr Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
title_full_unstemmed Direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
title_sort direct comparisons of inhibitor sensitivities of reverse transcriptases from feline and human immunodeficiency viruses.
publishDate 1990
url https://ncbi.nlm.nih.gov/pmc/articles/PMC171861/
https://ncbi.nlm.nih.gov/pubmed/1699491
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