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.

From: Role of water in cyclooxygenase catalysis and design of anti-inflammatory agents targeting two sites of the enzyme

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