Oligonucleotides containing modified bases. I. Inhibition of DNA and RNA polymerases by partially thiolated oligocytidylic acids.
A series of oligomers of cytidylic acid were prepared and partially (6-9% of the bases) thiolated in the 5 positions. The modified oligomers showed increasing inhibition with increasing chain length of both the DNA polymerase-alpha from regenerating rat liver and the DNA-dependent RNA polymerase of E. coli, but the minimum chain length for observable inhibitory activity was 5 nucleotide units for the DNA polymerase-alpha and 16 units for the RNA polymerase.
Ho
Y K
YK
Department of Medicinal Chemistry, State University of New York at Buffalo, Buffalo, NY 14214, USA.
Kung
M P
MP
Bardos
T J
TJ
D000818:Animals; D003568:Cytidine Monophosphate / Q000737:chemistry / Q000494:pharmacology*; D004256:DNA Polymerase I / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012321:DNA-Directed RNA Polymerases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000201:enzymology; D008099:Liver / Q000201:enzymology; D009841:Oligonucleotides / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013438:Sulfhydryl Compounds / Q000737:chemistry*
D004791:Enzyme Inhibitors; D009841:Oligonucleotides; D013438:Sulfhydryl Compounds; D012321:DNA-Directed RNA Polymerases; D004256:DNA Polymerase I; D003568:Cytidine Monophosphate