Table 1. Nucleotide and amino acid sequence of VHCDR2 and VLCDR1 and their mutants; IC50 and EC50 value tested on D54MG cells shown.
IC50 (ng/ml) |
EC50 (µM) |
|||||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Position: |
71 |
72 |
73 |
74 |
75 |
76 |
77 |
78 |
79 |
80 |
81 |
82 |
83 |
84 |
85 |
86 |
87 |
88 |
|
|
||
DmAb14-VHCDR2 Parental Amino Acid |
E |
I |
N |
P |
S |
N |
G |
R |
T |
N |
Y |
N |
E |
K |
F |
K |
S |
K |
N/A |
0.45 |
||
DmAb14-VHCDR2 Mutant# |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
||||
|
No.86 |
E |
I |
N |
P |
M |
D |
S |
R |
T |
N |
Y |
N |
E |
K |
F |
K |
S |
K |
N/A |
0.9 |
|
No.126 |
E |
I |
N |
P |
L |
P |
P |
R |
T |
N |
Y |
N |
E |
K |
F |
K |
S |
K |
N/A |
28 |
||
| ||||||||||||||||||||||
Position: |
25 |
26 |
27 |
28 |
29 |
30 |
31 |
32 |
33 |
34 |
35 |
36 |
37 |
38 |
39 |
|
|
|
|
|
||
DmAb14-VLCDR1# Parental Amino Acid |
R |
A |
S |
E |
S |
V |
E |
S |
Y |
G |
N |
N |
F |
M |
H |
|
|
|
N/A |
0.45 |
||
DmAb14-VLCDR1Mutant | ||||||||||||||||||||||
|
No. 23 |
R |
A |
R |
E |
A |
V |
E |
S |
Y |
G |
N |
N |
F |
M |
H |
|
|
|
N/A |
0.8 |
|
|
No.104 |
P |
W |
R |
E |
S |
V |
E |
S |
Y |
G |
N |
N |
F |
M |
H |
|
|
|
N/A |
4.7 |
|
No.184 | L | Y | G | E | S | V | E | S | Y | G | N | N | F | M | H | N/A | 0.2 |
# When VHCDR2 had mutations, VLCDR1 kept parental residues. When VLCDR1 had mutations, VHCDR2 kept parental residues. *Hot-spot positions are underlined and boldfaced.