Table 1 Interactions between GST-Syt II/Syt I and HCB variants measured by BLI

From: Engineered botulinum neurotoxin B with improved efficacy for targeting human receptors

Ligand

HCB

k on (M−1s−1)

k on error

k off (s−1)

k off error

K D (µM)

GST-m-Syt II

WT

1.47 × 104

5.89 × 102

1.98 × 10−3

5.18 × 10−5

0.13

GST-h-Syt II

WT

N/A

N/A

N/A

N/A

>20

 

E1191M

5.21 × 103

2.11 × 102

3.51 × 10−2

4.62 × 10−4

6.7

 

E1191M, S1199W

1.65 × 104

3.87 × 102

1.81 × 10−2

1.79 × 10−4

1.10

 

E1191M, S1199Y

1.56 × 104

3.72 × 102

1.13 × 10−2

1.74 × 10−4

0.72

 

E1191M, W1178Q

2.23 × 104

1.33 × 103

3.52 × 10−2

8.25 × 10−4

1.58

 

E1191C, S1199W

1.32 × 104

4.70 × 102

1.19 × 10−2

8.90 × 10−4

0.90

 

E1191C, S1199Y

1.47 × 104

4.96 × 102

1.44 × 10−2

1.91 × 10−4

0.98

 

E1191C, W1178Q

6.89 × 103

5.18 × 102

2.96 × 10−2

3.23 × 10−4

4.30

 

E1191Q, S1199W

8.28 × 103

5.50 × 102

2.21 × 10−2

3.34 × 10−4

2.67

 

E1191Q, S1199Y

2.42 × 104

1.16 × 103

2.85 × 10−2

4.60 × 10−4

1.18

 

E1191Q, W1178Q

N/A

N/A

N/A

N/A

>20

 

E1191V, S1199W

1.86 × 104

6.49 × 102

1.30 × 10−2

2.44 × 10−4

0.70

 

E1191V, S1199Y

2.31 × 104

9.18 × 102

1.35 × 10−2

2.68 × 10−4

0.59

 

E1191V, W1178Q

6.08 × 103

4.64 × 102

1.83 × 10−2

2.75 × 10−4

3.01

 

E1191M, S1199W, W1178Q

1.52 × 104

3.49 × 102

1.72 × 10−2

1.71 × 10−4

1.13

GST-h-Syt I

WT

N/A

N/A

N/A

N/A

>20

 

E1191M, S1199Y

4.82 × 103

2.96 × 102

1.40 × 10−2

4.55 × 10−4

2.90

 

E1191V, S1199Y

2.71 × 103

9.11 × 101

1.58 × 10−2

2.10 × 10−4

5.82

  1. Binding parameters were calculated using the Blitz system software. Representative binding and dissociation curves are shown in Supplementary Figs. 3 and 4