Table 2. Inhibition (KI in mM) by compound 3361 of d-glucose uptake mediated by a variety of hexose transporters.
| Transporter | KI for compound 3361 |
|---|---|
| PfHT Q169N | 0.271 ± 0.054 |
| PfHT 302AGT → SGL | 0.044 ± 0.018 |
| PfHT S302A | 0.064 ± 0.022 |
| PyHT | 0.080 ± 0.016 |
| PvHT | 0.112 ± 0.014 |
| PkHT | 0.108 ± 0.051 |
| TgGT1 | 2.073 ± 0.59 |
PyHT, P. yoelii hexose transporter; PvHT, P. vivax hexose transporter; PkHT, P. knowlesi hexose transporter; TgGT1, T. gondii glucose transporter. Mutants of PfHT are indicated individually. The KI value for the Q169N (helix 5) mutant was significantly (P < 0.001; multiple ANOVA with Bonferroni's correction) higher than for native PfHT (Table 1) and helix 7 mutants.