TABLE 2

IC50 and Ki values for BR and TR inhibition of [3H]uridine transport in yeast producing human nucleoside transporters Rates of transport of 1 μM [3H]uridine into yeast expressing pYPhENT1, pYPhENT2, pYPhCNT1, or pYphCNT3 were measured over 20 or 10 min in the presence of graded concentrations of BR and TR as described in Fig. 3. Mean IC50 ± S.E. values were determined using GraphPad Prism software version 3.0 and then converted to Ki values by the Cheng and Prusoff (1973) equation using Km values for uridine (Visser et al., 2002, 2004; Zhang et al., 2003).

Recombinant Transporter BR TR
IC50Ki IC50Ki
μM
hENT1 172 ± 21 168 ± 21 58 ± 5 57 ± 5
hENT2 272 ± 42 271 ± 42 16 ± 3 16 ± 3
hCNT1 224 ± 41 220 ± 40 225 ± 45 221 ± 44
hCNT3 252 ± 46 226 ± 41 6 ± 0.7 5.4 ± 0.6