Table 1. Substrate Km and active analogue Ki studies on native variants and mutants of PvHT.
Substrate or competitor | PfHT | PvHTind | PvHTind Q167N | PvHTind chimaera | PvHTsal |
---|---|---|---|---|---|
D-glucose | 1.0±0.2 (Km)* | 0.77±0.18 (Km)* | 0.60±0.12 (Km) | 0.65±0.24 (Km) | 0.52±0.13 (Km) |
D-fructose | 11.5±1.6 (Km)* | 19.03±4.4 (Ki) | 93.6±14.85 (Ki) | 17.05±2.76 (Ki) | 5.91±1.29 (Ki) |
2,5-AHM | 1.4±0.3 (Ki)* | 6.33±0.94 (Ki) | 10.19±0.89 (Ki) | 5.31±0.89 (Ki) | 1.48±0.45 (Ki) |
Compound 3361 | 0.053±0.02 (Ki)* | 0.12±0.01 (Ki)* | 0.52±0.09 (Ki) | 0.18±0.05 (Ki) | 0.13±0.01 (Ki) |
2-DOG | 1.3±0.3 (Km)* | 2.1±0.4 (Ki) | 1.81±0.2 (Ki) | 1.45±0.12 (Ki) | 1.24±0.24 (Ki) |
6-DOG | 2.2±0.9 (Ki)* | 11.74±3.04 (Ki) | 8.03±1.3 (Ki) | 10.52±2.43 (Ki) | 3.61±0.83 (Ki) |