TABLE 2.
Peptide sequence and IC50 values of wild type and alanine-mutated DOT1L peptides against AF9 and ENL proteins obtained by competitive SPR-based assay using CM5 chip with immobilized DOT1L protein
Peptide | Sequence | IC50 ± S.D. |
|
---|---|---|---|
AF9 | ENL | ||
μm | |||
DOT1L 10-mer | Ac-LPISIPLSTV-NH2 (amino acids 865–874) | 0.49 ± 0.22 | 1.34 ± 0.34 |
L865A | Ac-APISIPLSTV-NH2 | 98.5 ± 15.1 | 27.5 ± 6.8 |
P866A | Ac-LAISIPLSTV-NH2 | 3.3 ± 0.6 | 6.5 ± 1.2 |
I867A | Ac-LPASIPLSTV-NH2 | 57.2 ± 17.3 | >200 |
S868A | Ac-LPIAIPLSTV-NH2 | 5.3 ± 1.7 | 29.1 ± 0.8 |
I869A | Ac-LPISAPLSTV-NH2 | >200 | >200 |
P870A | Ac-LPISIALSTV-NH2 | 2.8 ± 0.1 | 11.6 ± 1.7 |
L871A | Ac-LPISIPASTV-NH2 | 30.7 ± 10.3 | 146.8 ± 11.5 |
S872A | Ac-LPISIPLATV-NH2 | 0.55 ± 0.21 | 2.8 ± 0.6 |
T873A | Ac-LPISIPLSAV-NH2 | 0.058 ± 0.017 | 0.36 ± 0.02 |
V874A | Ac-LPISIPLSTA-NH2 | 0.7 ± 0.02 | 4.2 ± 0.6 |
DOT1L 7-mer | Ac-LPISIPL-NH2 | 3.9 ± 0.1 | 7.3 ± 0.3 |
DOT1L 16-mer | Ac-LPISIPLSTVQPNKLP-NH2 (amino acids 865–880) | 0.32 ± 0.01 | 1.56 ± 0.09 |
AF4 14-mer | Ac- LMVKITLDLLSRIP-NH2 (amino acids 760–773) | 0.20 ± 0.06 | 0.43 ± 0.15 |