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Table 1 Second order rate constants ( k2) of inhibition for recombinant serpins

From: Fusion of the C-terminal triskaidecapeptide of hirudin variant 3 to alpha1-proteinase inhibitor M358R increases the serpin-mediated rate of thrombin inhibition

 

Serpin with M358R loop

Serpin with RCL5 loop

Protease

API M358R

HV3API

HAPI M358R

API RCL5

HV3 API RCL5

M358R

α-thrombin (×106 M-1 min-1)

22 ± 4

72 ± 15***

186 ± 32***

35 ± 8

66 ± 8***

γT-thrombin (×106 M-1 min-1)

5.9 ± 0.1

11 ± 3**

34 ± 10**

15 ± 0.8

21 ± 3***

APC (×106 M-1 min-1)

1.7 ± 0.1

1.9 ± 0.2

1.7 ± 0.2

0.0038 ± 0.0013a

0.022 ± 0.005***

α-thrombin/ APC ratio

13

39

109

9,211

3000

  1. Kinetic analysis of protease inhibition by API fusion proteins and variants. The mean of at least 5 k2 determinations ± SD is shown (×106 M-1 min-1). aValue from Sutherland et al., 2007. Values that are statistically significantly different from parent protein values (HV3API M358R and HAPI M358R compared to API M358R, HV3API RCL5 compared to API RCL5), **, p <0.01, ***, p < 0.001 by Mann–Whitney or two-tailed t test. Further details are provided in the text.