Table 3 Ki constants of human serine proteases inhibited by various APPI-3M variants

From: Mapping protein selectivity landscapes using multi-target selective screening and next-generation sequencing of combinatorial libraries

Mutant

aKi [pM]

Mesotrypsin

Anionic trypsin

Cationic trypsin

KLK6

Unmodified APPI-3M

98.0 ± 1.0

2.26 ± 0.08

22.5 ± 0.6

362 ± 10

T11V/G17R

494 ± 28

0.92 ± 0.07

2.37 ± 0.17

16.4 ± 0.9

T11S/G17R

1060 ± 30

2.98 ± 0.19

7.25 ± 0.5

124 ± 13

T11S

581 ± 7

1.16 ± 0.09

7.63 ± 0.55

1000 ± 60

T11V

65.0 ± 1.0

3.72 ± 0.21

14.1± 0.5

378 ± 9

G17R

676 ± 8

3.58 ± 0.16

8.12 ± 0.08

77.4 ± 2.6

  1. aResults (means ± SD) were obtained from three independent experiments
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