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. Author manuscript; available in PMC: 2020 May 31.
Published in final edited form as: J Med Chem. 2020 Mar 17;63(6):3298–3316. doi: 10.1021/acs.jmedchem.9b02078

Table 1.

Kinetic Parameters of Peptide Substances for Cruzaina

substrate structure kcat (s−1) Km (μM) kcat/Km (μM−1 s−1) kcat/Km rel kcat rel
S1 Cbz-Phe-Arg-AMC 9.6 ± 0.2 0.89 ± 0.09 11 ± 1 1.00 1.00
S2 Cbz-Phe-hPhe-AMC 2.0 ± 0.2 0.26 ± 0.06 8 ± 2 0.73 0.21
S3 Cbz-Leu-hPhe-AMC 3.0 ± 0.2 0.8 ± 0.2 4 ± 1 0.36 0.21
S4 Cbz-Leu-Arg-AMC 8.4 ± 0.4 2.2 ± 0.3 3.8 ± 0.7 0.35 0.88
S5 Cbz-Phe-(4-Pyr)Ala-AMC 7.5 ± 0.5 3.7 ± 0.5 2.0 ± 0.4 0.18 0.76
S6 Cbz-Arg-Arg-AMCb 7.2 ± 0.1 3.7 ± 0.4 1.9 ± 0.2 0.17 0.75
S7 NMePip-Phe-hPhe-AMC 4.0 ± 0.1 3.1 ± 0.3 1.3 ± 0.1 0.12 0.42
S8 Cbz-(4-Pyr)Ala-hPhe-AMC 5.3 ± 0.2 4.6 ± 0.5 1.1 ± 0.1 0.10 0.55
S9 Cbz-Phe-Phe-AMC 0.26 ± 0.01 0.34 ± 0.06 0.8 ± 0.2 0.07 0.03
S10 Cbz-Arg-hPhe-AMC 4.9 ± 0.1 6.8 ± 0.4 0.7 ± 0.04 0.06 0.51
S11 NMePip-Phe-Phe-AMC 2.8 ± 0.06 14 ± 4 0.2 ± 0.04 0.02 0.29
S12 Cbz-Phe-Ala-AMCb 0.89 ± 0.06 38 ± 2 0.023 ± 0.003 0.00 0.09
a

Data obtained at pH 7.5, 25 °C, and 10% DMSO (v/v).

b

Data obtained at 2% DMSO (v/v) from ref 40.