TABLE 4.
Summary of published results on P1 changes at HCV NS3-4A trans cleavage sites
Authors (yr) | Model | P1 residue | NS3 + NS4A
|
NS3 (no NS4A)
|
||||
---|---|---|---|---|---|---|---|---|
Km (μM) | kcat (min−1) | kcat/Km (M−1/s−1) | Km (μM) | kcat (min−1) | kcat/Km (M−1/s−1) | |||
Urbani et al. (1997) | E. coli-produced NS3 + NS4A-4B peptide | Cys | 43 ± 4 | 1 ± 0.1 | 545 | 105 ± 20 | 0.3 ± 0.03 | 48 |
hCysa | 54 ± 13 | 0.3 ± 0.01 | 96 | 312 ± 59 | 0.1 ± 0.01 | 5 | ||
Abue | 97 ± 29 | 0.17 ± 0.01 | 30 | 288 ± 30 | 0.03 ± 0.01 | 2 | ||
Thr | 235 ± 37 | 0.2 ± 0.01 | 15 | 244 ± 55 | 0.005 ± 0.001 | 0.3 | ||
Val | 153 ± 54 | 0.009 ± 0.001 | 1 | NDb | ND | ND | ||
Ser | NCd | NC | NC | NC | NC | NC | ||
Zhang et al. (1997) | Baculovirus-produced sc-NS3(1-631)/4A(1-54) + NS5A-5B peptide | Cysc | 30 | 8.9 | 5,000 | |||
hCysc | 70 | 1.0 | 240 | |||||
Alac | 240 | 0.5 | 35 | |||||
Thrc | 710 | 1.2 | 28 | |||||
Metc | 78 | 0.1 | 21 | |||||
Serc | 530 | 0.1 | 3 |
hCys, l-homocysteine.
ND, not determined (kcat/Km < 0.05 M−1 s−1).
Substrate was modified at the P2 position (Cys to Ala) to minimize synthesis and oxidation problems.
NC, no cleavage.
Abu, α-aminobutyric acid.