TABLE 1.
IC50 values and relative activities of lysine mutants against H. contortus and T. colubriformis
Mutant |
H. contortus |
T. colubriformis |
|||
---|---|---|---|---|---|
IC50 | Relative activitya | IC50 | Relative activitya | ||
μm | μm | ||||
Wild-type | kB1 | 2.7 | 1.0 | 4.5 | 1.0 |
Loop 1 | G6K | >11.5 | <0.2 | >11.5 | <0.4 |
E7K | >11.5 | <0.2 | >11.5 | <0.4 | |
T8K | >11.5 | <0.2 | >11.5 | <0.4 | |
Loop 2 | V10K | >11.5 | <0.2 | >11.5 | <0.4 |
G11K | 5.3 | 0.5 | 6.1 | 0.7 | |
G12K | >11.5 | <0.2 | >11.5 | <0.4 | |
T13K | 2.8 | 1.0 | 4.0 | 1.1 | |
Loop 3 | N15K | >11.5 | <0.2 | >11.5 | <0.4 |
T16K | >11.5 | <0.2 | >11.5 | <0.4 | |
P17K | 3.6 | 0.7 | 4.9 | 0.9 | |
G18K | 1.1 | 2.4 | 1.8 | 2.5 | |
Loop 4 | T20K | 0.9 | 3.0 | 1.7 | 2.6 |
Loop 5 | S22K | 2.3 | 1.1 | 2.7 | 1.7 |
W23K | >11.5 | <0.2 | >11.5 | <0.4 | |
P24K | N/Db | N/D | N/D | N/D | |
V25K | >11.5 | <0.2 | >11.5 | <0.4 | |
Loop 6 | T27K | 1.6 | 1.7 | 3.4 | 1.3 |
R28K | 3.9 | 0.7 | 7.7 | 0.6 | |
N29K | 0.4 | 7.0 | 1.2 | 3.8 | |
G1K | 0.5 | 5.8 | 1.5 | 2.9 | |
L2K | 6.2 | 0.4 | 6.6 | 0.7 | |
P3K | >11.5 | <0.2 | >11.5 | <0.4 | |
V4K | 11.1 | 0.2 | >11.5 | <0.4 | |
Double-lysine | T20K/S22K | 0.7 | 4.1 | 1.0 | 4.5 |
T20K/N29K | 0.4 | 6.5 | 0.7 | 6.8 | |
T20K/G1K | 0.4 | 6.5 | 0.7 | 6.8 | |
Triple-lysine | T20K/N29K/G1K | 0.2 | 13.0 | 0.7 | 6.2 |
a Expressed relative to wild-type kalata B1.
b N/D, not determined.