Table 1. Transport kinetics and inhibition.
| Protein | Inhibitor | KM (µM) | vmax* | Ki (µM) | α |
|---|---|---|---|---|---|
| Michaelis-Menten | Equation 2 | ||||
| hDMT1 | - | 3.1 ± 0.6 | 4.6 ± 0.3 | 0.57 ± 0.17 | >100 |
| 1 µM Br-DBFIT | 9.2 ± 1.2 | 4.2 ± 0.2 | |||
| 2.5 µM Br-DBFIT | 14.7 ± 2.8 | 4.3 ± 0.4 | |||
| 5 µM Br-DBFIT | 14.4 ± 3.0 | 3.4 ± 0.4 | |||
| hDMT1 | - | 2.6 ± 0.5 | 2.6 ± 0.1 | 0.35 ± 0.07 | 17.4 |
| 0.25 µM TMBIT | 4.0 ± 0.4 | 2.3 ± 0.1 | |||
| 0.5 µM TMBIT | 6.1 ± 0.8 | 2.4 ± 0.1 | |||
| 1.25 µM TMBIT | 8.0 ± 1.0 | 2.1 ± 0.1 | |||
| hDMT1 | - | 2.9 ± 0.4 | 3.1 ± 0.1 | 0.08 ± 0.01 | >100 |
| 0.25 µM TEBIT | 13.1 ± 3.3 | 3.0 ± 0.4 | |||
| 0.5 µM TEBIT | 18.3 ± 5.3 | 2.9 ± 0.5 | |||
| 1.25 µM TEBIT | 26.8 ± 8.6 | 2.5 ± 0.5 | |||
| hDMT1 | - | 2.6 ± 0.5 | 2.6 ± 0.1 | 3.6 ± 0.7 | 13.5 |
| 5 µM Br-BIT | 6.7 ± 0.7 | 2.4 ± 0.1 | |||
| 10 µM Br-BIT | 7.4 ± 1.2 | 2.2 ± 0.1 | |||
| 25 µM Br-BIT | 12.4 ± 3.7 | 1.6 ± 0.2 | |||
| hDMT1 S476V | - | 2.3 ± 0.5 | - | - | - |
| hDMT1 N520L | - | 2.4 ± 0.5 | - | - | - |
| hDMT1 F523A | - | 2.7 ± 0.6 | - | - | - |
| EcoDMT | - | 4.3 ± 0.5 | 21.9 ± 0.5 | 14.2 ± 2.6 | >100 |
| 10 µM Br-BIT | 13.7 ± 1.2 | 21.7 ± 0.4 | |||
| 50 µM Br-BIT | 21.7 ± 3.6 | 21.4 ± 1.0 | |||
| 100 µM Br-BIT | 31.5 ± 6.9 | 20.4 ± 1.3 | |||
| EcoDMT N456A | - | 12.5 ± 1.7 | 19.1 ± 0.6 | 29.3 ± 7.1 | 8.5 |
| 10 µM Br-BIT | 17.8 ± 4.0 | 18.3 ± 1.1 | |||
| 50 µM Br-BIT | 28.8 ± 5.4 | 14.9 ± 0.8 | |||
| 100 µM Br-BIT | 33.9 ± 6.9 | 13.8 ± 0.8 | |||
| EcoDMT N456L | - | 7.5 ± 0.7 | 17.3 ± 0.4 | 28.8 ± 5.3 | 29.2 |
| 10 µM Br-BIT | 13.1 ± 1.7 | 16.2 ± 0.5 | |||
| 50 µM Br-BIT | 19.0 ± 2.4 | 13.8 ± 0.5 | |||
| 100 µM Br-BIT | 27.0 ± 3.9 | 15.1 ± 0.6 | |||
| EcoDMT N456A S459A Q463A | 7.2 ± 0.9 | 21.9 ± 0.5 | 23.8 ± 3.2 | >100 | |
| 10 µM Br-BIT | 15.7 ± 1.7 | 21.7 ± 0.4 | |||
| 50 µM Br-BIT | 32.3 ± 4.5 | 21.4 ± 1.0 | |||
| 100 µM Br-BIT | 47.9 ± 5.6 | 20.4 ± 1.3 | |||
*νmax values for hDMT1 measurements are given in pmol min−1 well−1 and νmax values for EcoDMT measurements in ΔF Δt−1.