Table 2.
Summary of type and extent of inhibition for selected compounds against Leishmania mexicana arginase (LmARG) and human ARGI (HsARGI). The extent and type of inhibition for LmARG and HsARGI were determined by Dixon plot analysis or (for those marked with 'a') by calculation from panel data assuming the type of inhibition shown in the final column and using equations (1) and (2) (Section 2.8).
Inhibitor | Ki vs. LmARG | Ki vs. HsARGI | Type of Inhibition |
---|---|---|---|
ABH | 1.3 µM | 3.5 µM | Competitive |
BEC | ~10 µM | 14 µMa | Competitive |
nor-NOHA | ~50 µM* | ~10 µMa | Competitive |
NOHA | 85 µM | ~70 µMa | Competitive |
8-Aminoguanine | < 2 mM | N/A | Uncompetitive |
L-Cysteine | 11 mM | > 30 mMa | Competitive |
Trypanothione | < 5 mM | < 5 mMa | Uncompetitive |
ABH, 2(S)-amino-6-boronohaxanoic acid; BEC, S-(2-boronoethyl)-L-cysteine; nor-NOHA, Nω-Hydroxy-nor-L-arginine; NOHA, Nω-Hydroxy-L-arginine.