Table 1 Catalytic activity of COX-2 for AA metabolism in terms of PGE2 formation (ng/mL) and kinetic constants. Average of 3 expts, SD ± 0.5–2.0.
Entry | COX-2 | Activity % of wt COX-2 | Km (μM) | Kcat (s-1) | Kcat/Km (μM-1 s-1) |
---|---|---|---|---|---|
1 | wt | 100 | 4 | 55.2 | 13.8 |
2 | F381A | 93 | 8 | 45 | 5.6 |
3 | N382A | 67 | 6 | 35 | 5.8 |
4 | T383A | 40 | 10 | 28 | 2.8 |
5 | L384F | 36 | 12 | 25 | 2.0 |
6 | Y385F | 0 | 5 | 5.1 | 1.0 |
7 | H386V | 65 | 8 | 35 | 4.3 |
8 | H388V | 92 | 5 | 40 | 8 |
9 | T383A, H386V | 2 | 13 | 26 | 2 |
10 | H388V, H386V | 68 | 11 | 25 | 2.2 |