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. 2023 Jan 5;10:1089959. doi: 10.3389/fchem.2022.1089959

TABLE 4.

kapp values of selected alkyne and desthiobiotin probes against a panel of trypsin-like serine proteases and the description of the mechanism of inhibition defined by the progress curves: slow-binding (Rev.) or irreversible (Irrev.).

graphic file with name FCHEM_fchem-2022-1089959_wc_tfx30.jpg
# R1 R2 Alk/DtB a Trypsin-3 β-tryptase Thrombin uPA b CatG b
kapp (M−1 s−1) c
32b graphic file with name FCHEM_fchem-2022-1089959_wc_tfx31.jpg H Alk 18 × 102 ± 66 Irrev. 41 ± 5 Irrev. 64 ± 8 Rev. 41 ± 4 Irrev. * d Rev.
45b DtB 17 × 102 ± 122 Irrev. 237 ± 42 Irrev. 19 ± 2 Rev. N.D. N.D.
33b Cl Alk 35 × 102 ± 40 Irrev. 28 × 102 ± 82 Irrev. 11 × 102 ± 42 Rev. 15 × 102 ± 12 Irrev. * d Rev.
46b DtB 92 × 102 ± 349 Irrev. 75 × 102 ± 1475 Irrev. 63 × 102 ± 290 Rev. 940 ± 37 Irrev. N.D.
34b graphic file with name FCHEM_fchem-2022-1089959_wc_tfx32.jpg H Alk 40 × 103 ± 2642 Rev. 712 ± 41 Rev. 17 ± 1 Rev. 75 × 102 ± 725 Irrev. * d Rev.
50b DtB 49 × 103 ± 2979 Rev. 32 × 102 ± 613 Rev. 47 ± 5 Rev. 33 × 103 ± 12 × 103 Irrev. * d Rev.
35b NHCOCH3 Alk * d Rev. 70 × 102 ± 582 Rev. 128 ± 5 Rev. 13 × 104 ± 30 × 103 Irrev. 477 ± 67 Rev.
52b DtB 86 × 103 ± 8250 Rev. 18 × 103 ± 1184 Rev. 49 ± 5 Rev. 38 × 103 ± 4175 Irrev. * d Rev.
36b Cl Alk 29 × 103 ± 6499 Rev. 61 × 103 ± 6860 Rev. 251 ± 16 Rev. 32 × 104 ± 29 × 103 Irrev. * d Rev.
54b DtB * d Rev. * d Rev. * d Rev. 23 × 104 ± 36 × 103 Irrev. * d Rev.
37b graphic file with name FCHEM_fchem-2022-1089959_wc_tfx33.jpg H Alk 293 ± 34 Irrev. 375 ± 34 Irrev. N.D. 124 ± 23 Irrev. 582 ± 2 Irrev.
55b DtB 231 ± 18 Irrev. 347 ± 19 Irrev. N.D. 77 ± 1 Irrev. 301 ± 85 Irrev.
38b NHCOCH3 Alk 358 ± 6 Irrev. 20 × 102 ± 54 Irrev. N.D. 215 ± 7 Irrev. 14 × 102 ± 52 Irrev.
56b DtB 334 ± 85 Irrev. 321 ± 2 Irrev. N.D. 62 ± 2 Irrev. 420 ± 37 Irrev.
39b Cl Alk 11 × 102 ± 164 Irrev. 45 × 102 ± 547 Irrev. N.D. 25 × 102 ± 86 Irrev. 23 × 102 ± 347 Rev.
57b DtB 13 × 102 ± 340 Irrev. 65 × 102 ± 1,203 Irrev. N.D. 25 × 102 ± 11 Irrev. 11 × 102 ± 117 Rev.
41b graphic file with name FCHEM_fchem-2022-1089959_wc_tfx34.jpg H Alk 17 × 102 ± 142 Irrev. 27 ± 2 Irrev. 41 × 102 ± 38 Irrev. N.D. N.D.
31b Pro-Lys H Alk 13 × 102 ± 28 Irrev. 136 ± 3 Irrev. 13 × 102 ± 5 Irrev. 188 ± 1 Irrev. N.D.
a

Alk, alkyne probe; DtB, desthiobiotin probe.

b

Panel of serine proteases abbreviations: uPA, urokinase plasminogen activator; catG, cathepsin G.

c

kapp are calculated from two independent experiments; when SD was higher than three times the average value, a third independent experiment was run (mean ± SD).

d

kapp determination is not possible by curve fitting.

N.D.: IC50 is greater than 10 μM, and progress curves were not performed.