TABLE 3.
Cross-resistance of zanamivir-resistant or oseltamivir-resistant enzymes
| Residue in NA active centera and positionb | Amino acid | IC50 (nM)c
|
||
|---|---|---|---|---|
| RWJ-270201 | Oseltamivir carboxylate | Zanamivir | ||
| Framework | ||||
| 119 | Glu (wt)d | 1.1 | 0.4 | 2.5 |
| 119 | Gly | 1.8 | 0.5 | 100 |
| 119 | Ala | 1.6 | 1.1 | 50 |
| 119 | Asp | 9.5 | 0.5 | 150 |
| 274 | His (wt) | 0.5 | 1.0 | 1.0 |
| 274 | Tyr | 40 | 400 | 1.5 |
| Functional | ||||
| 292 | Arg (wt) | 1.1 | 0.4 | 2.5 |
| 292 | Lys | 30 | 3,750 | 20 |
| 152 | Arg (wt) | 1.4 | 4 | 3.5 |
| 152 | Lys | 570 | 750 | 100 |
a
According to Colman et al. (5).
b
Position of amino acid in the N2 enzyme.
c
IC50 in NA inhibition assays. The median IC50s of three or more measurements are shown.
d
Amino acid at the indicated position in the wild-type (wt) NA.