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. 2013 Nov 13;69(3):651–663. doi: 10.1093/jac/dkt442

Table 3.

Kinetic parameters of high-affinity and low-affinity pentamidine transport in various strains of T. b. brucei bloodstream forms and in Leishmania mexicana expressing TbAQP2

Strain HAPT1 pentamidine Km (μM) HAPT1 propamidine Ki (μM) HAPT1 diminazene Ki (μM) LAPT1 pentamidine Km (μM)
WT s427a 0.036 ± 0.006 4.6 ± 0.7 63 ± 3 56 ± 8
TbAT1-KOb 0.029 ± 0.008 13.0 ± 3.0 ND 50 ± 17
B48c NP 56 ± 7
P1000 NP 99 ± 24
B48/AQP2 0.046 ± 0.014 15.2 ± 1.6 ND 66 ± 1
L. mexicana/TbAQP2 0.055 ± 0.004 8.1 ± 0.8 100 ± 21 not present in these cells

ND, not determined; NP, not present in these cells.

In the B48 and P1000 strains, no high-affinity transport of pentamidine was detectable, nor was pentamidine uptake inhibited by propamidine.

aDe Koning.17

bMatovu et al.14

cBridges et al.16