Table 2. Kinetic constants for hPCFT.
Kinetic constants for MTX (Kt and Vmax) were determined with [3H]MTX by Lineweaver-Burke plots with R2/hPCFT4 cells, whereas Ki values were determined by Dixon plots with [3H]MTX as substrate and a range of inhibitor concentrations in R2/hPCFT4 cells. Results are presented as mean values ± standard errors from 3 experiments.
| Substrate | Parameter | pH 5.5 | pH 6.8 |
|---|---|---|---|
| MTXa | Kt (micromolar) | 0.28 ± 0.02 | 4.52 ± 0.19 |
| MTXa | Vmax (pmol/mg/min) | 31.23 ± 4.31 | 13.72 ± 2.26 |
| PMXa | Ki (micromolar) | 0.096 ± 0.012 | 1.54 ± 0.17 |
| 3 | Ki (micromolar) | 0.13 ± 0.01 | 1.82 ± 0.07 |
| 4a | Ki (micromolar) | 0.13 ± 0.01 | 1.95 ± 0.02 |
From Wang et al. (ref. 14).