TABLE 1.
Ki values for 5-methylTHF, 5-formylTHF, and folic acid based upon inhibition of 0.5 μm [3H]MTX influx
Ki values are the mean ± S.E. from three independent experiments. The [3H]MTX concentrations were comparable to the Kt for each carrier, and the concentrations of inhibitors were adjusted so that inhibition achieved was in the 35–65% range.
ki |
|||
---|---|---|---|
5-formylTHF | 5-methylTHF | Folic acid | |
μm | |||
WT-PCFT | 1.17 ± 0.12 | 0.67 ± 0.21 | 1.63 ± 0.18 |
H247A | 0.17 ± 0.02 | 0.20 ± 0.01 | 0.20 ± 0.02 |