Table 1 Binding EC50 values (ELISA and flow cytometry) and cytotoxic effects of the scTRAIL-antibody fusion proteins to their target antigens DR5 and EGFR and EGFR-positive cell lines Colo205 and HCT116. n = 3; mean ± sd; -: not performed.

From: Comparison of antibody-scTRAIL Fc fusion proteins with varying valency for EGFR and TRAIL receptors

Moieties

Mole-

cule

Format

ELISA

Cell binding

Cytotoxicity

DR5

EGFR

Colo205

HCT116

Colo205

HCT116

Fab/scFv + scTRAIL

EC50 [pM]

EC50 [pM]

EC50 [pM]

EC50 [pM]

EC50 [pM]

Maximal killing [%]

EC50 [pM]

Maximal

killing [%]

0 + 2

#1

Fc-scTRAIL

493 ± 53

-

5,173 ± 3,085

3,850 ± 990

36 ± 4

100

71 ± 30

75

0 + 2

#7

scTRAIL-Fc

383 ± 64

-

4,411 ± 1,725

6,177 ± 1,027

52 ± 4

100

177 ± 24

75

2 + 2

#3

IgG-scTRAIL

655 ± 145

291 ± 58

86 ± 20

129 ± 25.8

6 ± 1

100

6 ± 2

75

2 + 2

#4

scFv-Fc-scTRAIL

434 ± 22

496 ± 232

244 ± 141

351 ± 46

6 ± 1

100

8 ± 2

75

2 + 2

#9

scTRAIL-Fc-scFv

1,069 ± 124

768 ± 142

997 ± 349

633 ± 134

9 ± 2

100

12 ± 6

75

2 + 1

#5

IgG-scTRAIL

1,268 ± 456

211 ± 34

51 ± 20

352 ± 274

1,756 ± 1076

25

256 ± 142

50

2 + 1

#6

scFv-Fc-scTRAIL

753 ± 71

2,344 ± 16

73 ± 22

188 ± 147

1,536 ± 1155

38

499 ± 276

55

1 + 1

#11

scFv-scTRAIL-Fc

883 ± 381

767 ± 28

258 ± 123

1,492 ± 999

418 ± 211

50

472 ± 60

60

1 + 1

#10

Fab-scTRAIL-Fc

929 ± 185

1,641 ± 144

255 ± 23

746 ± 65

1,385 ± 449

50

727 ± 43

60

0 + 1

#2

DIgG-Fc-scTRAIL

1,283 ± 295

-

3,153

72,000

601 ± 75

100

844 ± 445

70

0 + 1

#8

DFab-scTRAIL-Fc

853 ± 208

-

5,680

18,000

139 ± 42

100

264 ± 141

70