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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.