(s4dU)35: a novel, highly potent oligonucleotide inhibitor of the human immunodeficiency virus type 1 reverse transcriptase

FEBS Letters

Aradi, Janos¹  Tökés, Szilvia¹ 

[1] Department of Biochemistry, University Medical School of Debrecen, P.O. Box 6, H-4012 Debrecen, Hungary

关键词: Inhibition;    Reverse transcriptase;    Human immunodeficiency virus;    Oligo 4-thio-2′-deoxyuridylate;    Antitemplate;    RT;    reverse transcriptase;    HIV;    human immunodeficiency virus;    AIDS;    acquired immunodeficiency syndrome;    TCA;    trichloroacetic acid;    Na-PPi;    Na-pyrophosphate;   

DOI  :  10.1016/0014-5793(96)01032-0

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Oligodeoxycytidylates were converted to s⁴dUMP-containing oligomers by treatment with liquid H₂S. The inhibitory potency of the modified oligonucleotides on human immunodeficiency virus type 1 reverse transcriptase depended on the chain length and on the percentage of modification. The most potent reverse transcriptase inhibitor was (s⁴dU)₃₅. The inhibitory pattern was competitive, when either poly(A)·(dT)₁₆ or poly(C)·(dG)₁₆ was used as template-primer (variable substrate), suggesting that the free enzyme interacts with (s⁴dU)₃₅. The K _i values were 3.0 and 2.2 nM in the presence of poly(A)·(dT)₁₆ and poly(C)·(dG)₁₆, respectively.

【 授权许可】

Unknown