(s4dU)35: a novel, highly potent oligonucleotide inhibitor of the human immunodeficiency virus type 1 reverse transcriptase.
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) x (dT)16 or poly(C) x (dG)l6 was used as template-primer (variable substrate), suggesting that the free enzyme interacts with (s4dU)35. The Ki values were 3.0 and 2.2 nM in the presence of poly(A) x (dT)16 and poly(C) x (dG)16, respectively.
Tökés
S
S
Department of Biochemistry, University Medical School of Debrecen, Hungary.
Aradi
J
J
D002851:Chromatography, High Pressure Liquid; D017931:DNA Primers; D003856:Deoxyuracil Nucleotides / Q000737:chemistry*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D009841:Oligonucleotides / Q000737:chemistry* / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry
D017931:DNA Primers; D003856:Deoxyuracil Nucleotides; D009841:Oligonucleotides; D018894:Reverse Transcriptase Inhibitors; D013455:Sulfur; C007267:2'-deoxyuridylic acid; D054303:HIV Reverse Transcriptase