Table 1. Percent inhibition by MIPS2673 of PfA-M1 and PvA-M1 aminopeptidase activities compared to selected human M1 homologues.
Concentration (µM) | % inhibition* | ||||
---|---|---|---|---|---|
PfA-M1 | PvA-M1 | LTA4H | ERAP1 | ERAP2 | |
1.25 | 100 | 100 | 0 | 0 | 31 |
10 | 100 | 100 | 58 | 2.3 | 0 |
500 | – | – | 42.2 | 89.8 | 97.8 |
1000 | – | – | 53.4 | 95.6 | 98.7 |
Values represent the mean of three independent experiments. All assays were performed at pH 8.0. The concentration of substrate H-Leu-NHMec (H-Leu-NHMec, L-leucine-7-amido-4-methylcoumarin hydrochloride) varied depending on the enzyme assayed 20 µM for PfA-M1, 40 µM for PvA-M1, and 100 µM for ERAP1 and ERAP2. LTA4H was assessed using the substrate H-Ala-NHMec (L-alanine-7-amido-4-methylcoumarin hydrochloride) at a concentration of 20 µM. LTA4H, leukotriene A-4 hydrolase. ERAP1, endoplasmic reticulum aminopeptidase 1. ERAP2, endoplasmic reticulum aminopeptidase 2.