Table 1.
1 AZ Variants | Location | 2 IC50 (μM) |
3 Fold Change (IC50,mutant/IC50,WT) |
---|---|---|---|
AZ95–228 | C-terminal domain | 0.16 ± 0.01 | 1 |
AZ95–228_E142A | β5 | 0.31 ± 0.02 | 1.93 |
AZ95–228_K153A | α1 | 0.40 ± 0.10 | 2.5 |
AZ95–228_D154A | α1 | 0.27 ± 0.06 | 1.69 |
AZ95–228_E161A | α1 | 0.25 ± 0.06 | 1.56 |
AZ95–228_E164A | α1 | 0.30 ± 0.06 | 1.88 |
AZ95–228_E165A | α1 | 0.30 ± 0.07 | 1.88 |
AZ95–228_H171A | β6 | 0.27 ± 0.09 | 1.69 |
AZ95–228_K178A | Loop between β6 and α2 | 0.31 ± 0.05 | 1.94 |
AZ95–228-3Mα1 | α1 | 4.13 ± 0.34 | 25.82 |
AZ95–228-3Mα1_D154A | α1 | 5.61 ± 0.35 | 35.08 |
AZ95–228-3Mα1_E161A | α1 | 6.31 ± 5.95 | 39.45 |
AZ95–228-5Mα1 | α1 | No Inhibition | - |
AZ95–228-3Mα1_E142A | α1/β5 | No Inhibition | - |
AZ95–228-3Mα1_H171A | α1/β6 | No Inhibition | - |
AZ95–228-3Mα1_K178A | α1/loop_β6-α2 | No Inhibition | - |
AZ95–228_E142A/H171A/K178A | β5/β6/loop_β6-α2 | No Inhibition | - |
AZ95–228-8M | β5/α1/β6/loop_β6-α2 | No Inhibition | - |
1 AZ95–228-3Mα1: AZ95–228_K153A/E164A/E165A, AZ95–228-5Mα1: AZ95–228_K153A/D154A/E161A/E164A/E165A, AZ95–228-8M: AZ95–228_E142A/K153A/D154A/E161A/E164A/E165A/H171A/K178A. 2 All IC50 values were derived from fitting the inhibition curves of ODC shown in Figure 2 and Figure S2. 3 Fold change was the ratio of IC50 of the mutant versus IC50 of WT.