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. Author manuscript; available in PMC: 2019 Mar 12.
Published in final edited form as: J Med Chem. 2017 Apr 19;60(9):3814–3827. doi: 10.1021/acs.jmedchem.7b00018

Table 2. Inhibition of MMPs by GlyΨ{PO2H-CH2}Ile THPIs.

enzyme inhibitor Ki (nM)
MT1-MMP GlyΨ{PO2H-CH2}Ile-His-Lys-Gln THPI 4704 ± 708.4
MMP-8 GlyΨ{PO2H-CH2}Ile-His-Lys-Gln THPI 124.6 ± 6.9
MMP-1 GlyΨ{PO2H-CH2}Ile-His-Lys-Gln THPI 169.2 ± 28.4
MMP-3 GlyΨ{PO2H-CH2}Ile-His-Lys-Gln THPI NIa
MT1-MMP GlyΨ{PO2H-CH2}Ile-Tyr-Phe-Gln THPI 46.15 ± 4.7
MMP-1 GlyΨ{PO2H-CH2}Ile-Tyr-Phe-Gln THPI 110.59 ± 29.8
MMP-2 GlyΨ{PO2H-CH2}Ile-Tyr-Phe-Gln THPI 17.82 ± 1.9
MMP-3 GlyΨ{PO2H-CH2}Ile-Tyr-Phe-Gln THPI 13600.33 ± 5160.7
MMP-8 GlyΨ{PO2H-CH2}Ile-Tyr-Phe-Gln THPI 62.1 ± 2.5
MMP-9 GlyΨ{PO2H-CH2}Ile-Tyr-Phe-Gln THPI 0.03 ± 0.02
MMP-13 77.13 ± 14.4
a

NI = no inhibition at a THPI concentration of 1000 nM.