Table 2.
Relative proportions of ketose forms and active analogue studies on PfHT1 and GLUT1
| Substrate | % furanose
|
% pyranose
|
PfHT1Ki | GLUT1 Ki | ||
|---|---|---|---|---|---|---|
| α | β | α | β | |||
| d-Fructose | 6.5 | 25 | 2.5 | 65 | Km = 11.5* ± 1.6, Ki = 10.6, 11.7 | >50 |
| C2 position | ||||||
| 2,5-AHM | 100 | 1.4 ± 0.3* | >50 | |||
| C3 position | ||||||
| d-Psicose | 39 | 15 | 22 | 24 | >50 | ND |
| C4 position | ||||||
| d-Tagatose | 2.5 | 7.5 | 71 | 18 | >50 | ND |
| C5 position | ||||||
| l-Sorbose | 4 | 1 | 93 | 2 | >50 | ND |
| C6 position | ||||||
| d-Xylulose | 63 | 20 | — | — | >50 | ND |
Values are in mM unless otherwise indicated. Independent replicate Ki values based on inhibition of d-glucose uptake are shown. Proportions of different forms are from published work (29). The proportion of acyclic carbonyl forms is omitted.
*Means ± SE of three independent experiment