TABLE 1

Inhibition of clonogenicity (LC50) by l-configuration nucleoside analogs and d-configuration nucleoside analogs in RKO cell lines with under- or over-expression of APE-1 protein

LC50 was defined as the concentration of drug to give 50% of surviving fraction, and values are means ± S.D. of three experiments, with each data point done in triplicate.

Inhibition of Clonogenicity LC50
Cell Line with Transfection l-Configuration d-Configuration
Dox (100 ng/ml) l-OddC l-Fd4C dFdC AraC
nM μM nM nM
Con ShRNA 158 ± 18 5.4 ± 1.8 2.4 ± 0.5 16.5 ± 3.5
+ 163 ± 19 5.9 ± 2.3 2.5 ± 0.7 15 ± 4.5
shRNA 119 ± 20 6.1 ± 1.1 3.2 ± 1.1 20.7 ± 4.7
+ 56 ± 5 3.2 ± 0.9 3.4 ± 1.2 21.7 ± 5.6
Con pcDNA5 125 ± 35 5.5 ± 0.7 2.5 ± 0.6 12.2 ± 3.8
+ 128 ± 25 6.5 ± 0.6 2.6 ± 0.8 13 ± 2.8
Wt-APE-1 108 ± 25 4.3 ± 1.2 2.5 ± 0.4 16.5 ± 6.5
+ 238 ± 53 9.2 ± 2.7 2.6 ± 0.3 17.5 ± 2.5
C65A-APE-1 158 ± 25 5.6 ± 1.4 2.5 ± 0.1 18.5 ± 3.5
+ 263 ± 18 10.9 ± 2.3 2.7 ± 0.2 21 ± 1.4
E96A-APE-1 123 ± 4 4.5 ± 0.4 2.5 ± 0.1 14 ± 5
+ 130 ± 7 4.3 ± 0.5 2.6 ± 0.1 15 ± 6
E96Q-APE-1 140 ± 27 4.9 ± 0.5 2.4 ± 0.3 19 ± 3
+ 133 ± 19 5.2 ± 0.3 2.2 ± 0.2 17 ± 5