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(s 4dU) 35: a novel, highly potent oligonucleotide inhibitor of the human immunodeficiency virus type 1 reverse transcriptase

Oligodeoxycytidylates were converted to s 4dUMP-containing oligomers by treatment with liquid H 2S. 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...

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Published in:FEBS letters 1996-10, Vol.396 (1), p.43-46
Main Authors: Tökés, Szilvia, Aradi, Janos
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Language:English
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description Oligodeoxycytidylates were converted to s 4dUMP-containing oligomers by treatment with liquid H 2S. 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 (s 4dU) 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 (s 4dU) 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.
doi_str_mv 10.1016/0014-5793(96)01032-0
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ispartof FEBS letters, 1996-10, Vol.396 (1), p.43-46
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1873-3468
language eng
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source ScienceDirect Journals
subjects AIDS, acquired immunodeficiency syndrome
AIDS/HIV
Antitemplate
Chromatography, High Pressure Liquid
Deoxyuracil Nucleotides - chemistry
DNA Primers
HIV Reverse Transcriptase - antagonists & inhibitors
HIV, human immunodeficiency virus
Human immunodeficiency virus
Inhibition
Na-PPi, Na-pyrophosphate
Oligo 4-thio-2′-deoxyuridylate
Oligonucleotides - chemistry
Oligonucleotides - pharmacology
Reverse transcriptase
Reverse Transcriptase Inhibitors - chemistry
Reverse Transcriptase Inhibitors - pharmacology
RT, reverse transcriptase
Structure-Activity Relationship
Sulfur - chemistry
TCA, trichloroacetic acid
title (s 4dU) 35: a novel, highly potent oligonucleotide inhibitor of the human immunodeficiency virus type 1 reverse transcriptase
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