Figure 4
From: Design of substrate-based BCR-ABL kinase inhibitors using the cyclotide scaffold
Inhibition of Abl kinase activity induced by MTAbl peptides determined using the BacKin assay.
(a) The percentage of Abl kinase (0.2 U/mL) inhibition in the presence of 32 μM of each peptide at 37 °C for 30 min. MTAbl peptides that have significant difference in inhibition efficacy compared to abltide are marked with asterisks (****p < 0.0001; ***p < 0.001, evaluated with one-way ANOVA). (b) Inhibition of Abl kinase activity induced by increasing concentrations of IM, MTAbl13 or MTAbl14. MTAbl13* corresponds to inhibition of [T315I]Abl kinase. Data were fitted to a sigmoidal dose-response curve with variable slope model and analyzed with GraphPad Prism 6. Results shown here are the mean ± SEM from two independent experiments.
