Details

Autor(en) / Beteiligte

• Cheng, Y.C.
• Dutschman, G.E.
• Bastow, K.F.
• Sarngadharan, M.G.
• Ting, R.Y.

Titel

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

Ist Teil von

• The Journal of biological chemistry, 1987-02, Vol.262 (5), p.2187-2189

Ort / Verlag

Bethesda, MD: Elsevier Inc

Erscheinungsjahr

1987

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.