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. 2019 Dec 5;8:e51913. doi: 10.7554/eLife.51913

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.