Table 1. Mapping non-template antisense region for the inhibition of telomerase activity.
Phosphoramidate oligonucleotides were pre-incubated with purified telomerase extract at concentrations ranging from 0.2–125 nM. Primer [100 nM d(TTAGGG)3] and nucleotides [10 µM dATP (50 c.p.m./fmol [α-33P]dATP), 50 µM dGTP, 200 µM dTTP] were added and the reactions were incubated for 90 min at 37°C. Enzymatic activity was measured by determining the rate of nucleotide addition to primer as assessed by the incorporation of [α-33P]dATP into acid insoluble counts. Dose-response curves as shown in Figure 1 were used to derive the concentration where 50% inhibition occurred (IC50).
*Compete inhibition was not reached even at concentrations over 100 nM; partial inhibition (20–50%) was observed in the low nanomolar range.