Table 3.
DADMe-ImmH
|
ImmH
|
5′-deoxy-ImmH
|
||||||||
---|---|---|---|---|---|---|---|---|---|---|
Ki*a |
Km/Ki |
Ki | Ki* |
Km/Ki |
Kib |
Km/Ki |
||||
Enzyme | Value | Fold | Value | Fold | Value | Fold | ||||
Native | 10.7 ± 1.1 pM | 3,700,000 | 1 | a | 57.9 ± 1.5 pM | 690,000 | 1 | 20.0 ± 0.9 nM | 2,000 | 1 |
His257Phe | 950 ± 60 pM | 337,000 | 11 | 172 ± 16 nM | b | 1,860 | 370 | 19.8 ± 1.0 nM | 16,200 | 8 |
His257Gly | 270 ± 20 pM | 2,800,000 | 1 | 11.0 ± 0.9 nM | b | 68,100 | 10 | 7.7 ± 0.6 nM | 97,000 | 93 |
His257Asp | 900 ± 100 pM | 1,500,000 | 2 | 86 ± 7 nM | b | 15,700 | 45 | 54 ± 3 nM | 25,000 | 12 |
The weak inhibition phase (Ki) was observed but too short to quantitate, so only the slow-onset, tight-binding phase (Ki*) is reported.
No slow-onset phase was observed.