Table 1.
Active analogue and Km studies on PfHT1 and GLUT1
| Substrate | PfHT1Ki | GLUT1 Ki |
|---|---|---|
| Aldose analogues | ||
| d-Glucose | Km = 1.0 ± 0.2* | Km = 2.3, 2.6 |
| C1 position | ||
| 1-Deoxy-d-glucose | 14.7, 15.9 | 38.8, >50 |
| 1F-1-α-Deoxy-d-glucose | 1.0, 1.6 | 1.3, 1.7 |
| 1F-1-β-Deoxy-d-glucose | 1.0, 2.4 | 1.0, 5.2 |
| 1α-1-Methylglucopyranoside | >50 | ND |
| 1β-1-Methylglucopyranoside | >50 | ND |
| C2 position | ||
| 2-Deoxy-d-glucose | Km = 1.3 | 3.1, 6.3 |
| 0.9, 1.7 | ||
| d-Mannose | 0.7, 1.1 | 1.4, 3.5 |
| C3 position | ||
| 3-Deoxy-d-glucose | 13.2, 16.8 | >50 |
| 3-OMG | Km = 1.3 ± 0.3* | 30.8, 36.9 |
| Ki = 1.4, 2.7 | ||
| 3-Fluoro-3-deoxy-d-glucose | 1.6, 1.8 | ND |
| d-Allose | 22.0, 25.3 | >50 |
| C4 position | ||
| d-Galactose | 6.1, 7.9 | 25.2, 47.1 |
| 4,6-O-Ethylidene-α-d- glucose | >50 | ND |
| C5 position | ||
| 5-Thio-d-glucose | 2.7, 3.7 | 4.6, 6.9 |
| C6 position | ||
| 6-Deoxy-d-glucose | 2.2 ± 0.9* | 15.0, 16.8 |
| d-Xylose | 16.1, 34.4 | >50 |
| Endofacial ligand | ||
| Cytochalasin B | 1.4, 4.3 μM | 0.9 μM |
| Miscellaneous† | >50 | ND |
Values are in mM unless otherwise indicated. Independent replicate Ki values based on inhibition of d-glucose uptake are shown. The 6-DOG value for PfHT1 has been previously reported (2).
*
Means ± SE of three independent experiments.
†
Consists of d-mannitol, d-sorbitol, myo-inositol, sucrose, dehydroascorbic acid, glucose 6-phosphate, and maltose.