Table 1 Structures and in vitro activities of pepstatin and analogues.
From: Esterase mutation is a mechanism of resistance to antimalarial compounds
Compound | Structure | Potency* (ÎĽM) |
|---|---|---|
Pepstatin (P) | Iva-Val-Val-Sta-Ala-Sta-OH | none at 40 |
Acetyl pepstatin | Ac-Val-Val-Sta-Ala-Sta-OH | none at 20 |
Pepstatin-Penetratin | Pepstatin-RQIKIWFQNRRMKWKK-OH | none at 1 |
Pepstatin n-butyl amide | Pepstatin-CO-NH-(CH2)3CH3 | none at 20 |
Pepstatin methyl ester (PME) | Pepstatin-COO-CH3 | 5.12±0.15 |
Pepstatin ethyl ester (PEE) | Pepstatin-COO-CH2-CH3 | 0.730±0.012 |
Pepstatin 3-methyl-1-butyl ester (PMBE) | Pepstatin-COO-(CH2)2CH-(CH3)2 | 0.071±0.010 |
Pepstatin n-butyl ester (PBE) prep 1 | Pepstatin-COO-(CH2)3-CH3 | 0.083±0.006 |
Pepstatin n-butyl ester (PBE) prep 2 | Pepstatin-COO-(CH2)3-CH3 | 0.092±0.006 |
Pepstatin n-hexyl ester (PHE) prep 1 | Pepstatin-COO-(CH2)5-CH3 | 0.019±0.003 |
Pepstatin n-hexyl ester (PHE) prep 2 | Pepstatin-COO-(CH2)5-CH3 | 0.026±0.003 |
