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. 2013 Sep 1;288(42):30585–30596. doi: 10.1074/jbc.M113.457135

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
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