Recognition of structure of 5-halogenated derivatives of ara-UTP by DNA polymerase gamma and reverse transcriptase.
This report deals with the test of a series of 5-halogenated derivatives of ara-UTP for the inhibition of DNA polymerase gamma and viral reverse transcriptase. The compounds newly synthesized and tested were; ara5-FUTP, ara5-C1UTP, ara5-BrUTP and ara5-IUTP. The results were: 1) All these compounds were inhibitory to DNA polymerase gamma and reverse transcriptase. The mode of inhibitions was, in all cases, competitive against dTTP. 2) Ki values for these inhibitors with DNA polymerase gamma were lower than those with reverse transcriptase. 3) Ara5-ClUTP was less inhibitory to reverse transcriptase than other derivatives.
D000818:Animals; D001088:Arabinonucleotides / Q000494:pharmacology; D004258:DNA Polymerase III / Q000037:antagonists & inhibitors*; D006219:Halogens; D007700:Kinetics; D051379:Mice; D019384:Nucleic Acid Synthesis Inhibitors; D010954:Plasmacytoma; D011925:Rauscher Virus / Q000201:enzymology; D018894:Reverse Transcriptase Inhibitors; D013329:Structure-Activity Relationship; D014500:Uracil Nucleotides / Q000031:analogs & derivatives / Q000494:pharmacology; D014544:Uridine Triphosphate / Q000031:analogs & derivatives / Q000494:pharmacology
D001088:Arabinonucleotides; D006219:Halogens; D019384:Nucleic Acid Synthesis Inhibitors; D018894:Reverse Transcriptase Inhibitors; D014500:Uracil Nucleotides; C025327:ara-UTP; D004258:DNA Polymerase III; D014544:Uridine Triphosphate