Human immunodeficiency virus reverse transcriptase. General properties and its interactions with nucleoside triphosphate analogs. NLM AIDSLINE Important note: Information in this article was accurate in 1987. The state of the art may have changed since the publication date.

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Human immunodeficiency virus reverse transcriptase. General properties and its interactions with nucleoside triphosphate analogs.

J Biol Chem. 1987 Feb 15;262(5):2187-9. Unique Identifier : AIDSLINE MED/87137442
Cheng YC; Dutschman GE; Bastow KF; Sarngadharan MG; Ting RY

Abstract: Using affinity purified human immunodeficiency virus (HIV) reverse transcriptase the reaction assay conditions were determined. The optimum incorporation of dTMP into the (rA)n(dT)10 template with HIV reverse transcriptase required 6 mM MgCl2 and 80 mM KCl. The template specificity of HIV reverse transcriptase is quite different from those of the human gamma-polymerase-associated reverse transcriptase or avian virus reverse transcriptase. The preferential inhibition of HIV reverse transcriptase as compared to human gamma-reverse transcriptase was observed with several nucleoside analog triphosphates. The Ki values for thymidine triphosphate analogs with HIV reverse transcriptase ranged from 5 to 13 nM with decreasing effectiveness for 3'-fluoro greater than 3'-amino greater than 2',3'-dideoxy greater than 3'-azido groups. This study provides information on the structure activity relationships of the triphosphate analogs inhibitory effects on HIV reverse transcriptase versus human gamma-polymerase-associated reverse transcriptase, and the possible mechanisms of action of 3' azido thymidine and the 2',3'-dideoxynucleosides, and also identifies other nucleoside analogs for possible development as inhibitors of HIV.
Keywords: Deoxyguanine Nucleotides/METABOLISM Human HIV/*ENZYMOLOGY Kinetics Molecular Weight Nucleotides/*METABOLISM Reverse Transcriptase/*METABOLISM Structure-Activity Relationship Substrate Specificity Support, Non-U.S. Gov't Support, U.S. Gov't, P.H.S. Thymine Nucleotides/METABOLISM JOURNAL ARTICLE

KWDdeoxyguaninenucleotides/metabolismhumanhiv/KWDenzymologykineticsmolecularweightnucleotides/KWDmetabolismreversetranscriptase/KWDmetabolismstructure-activityrelationshipsubstratespecificitysupport,non-uKWDsKWDgov'tsupport,uKWDsKWDgov't,pKWDhKWDsKWDthyminenucleotides/metabolismjournalarticle
870630
M8760190

Copyright © 1987 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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