Table 4. Effect of 5 complete inhibitor peptide variants on 10 human kinases.
Peptide sequence | WLRRIKA- WLRRIKA- LNRQLGVAA |
YARA- AARQARAKA- LNRQLGVAA |
FAK- LAARLYRKA- LARQLGVAA |
KAFAK- LAARLYRKA- LARQLGVAA |
YARA- AARQARAKA- LARQLGVAA |
---|---|---|---|---|---|
Concentration of peptide inhibitor (μM) | 30 | 300 | 100 | 100 | 300 |
Human kinase | Percentage kinase activity | ||||
MK2 | 2 ± 1 | 10 ± 3 | 5 ± 2 | 8 ± 1 | 0 ± 0 |
MK3 | 16 ± 2 | 19 ± 3 | 10 ± 1 | 17 ± 1 | 5 ± 1 |
CaMKI | 9 ± 1 | 8 ± 1 | 0 ± 2 | 0 ± 2 | 2 ± 0 |
MK5 | 67 ± 9 | 81 ± 3 | 131 ± 4 | 148 ± 4 | 86 ± 2 |
SAPK2a (p38α) | 61 ± 7 | 100 ± 6 | 30 ± 6 | 59 ± 8 | 66 ± 3 |
IRAK4 | 12 ± 1 | 68 ± 3 | 13 ± 4 | 16 ± 2 | 23 ± 2 |
MLCK | 4 ± 1 | 66 ± 9 | 1 ± 1 | 2 ± 0 | 9 ± 0 |
PKBβ | 18 ± 2 | 96 ± 1 | 16 ± 5 | 28 ± 4 | 17 ± 2 |
PKCδ | 11 ± 0 | 105 ± 2 | 40 ± 2 | 24 ± 3 | 101 ± 3 |
ROCK-I | 0 ± 1 | 95 ± 7 | 25 ± 2 | 29 ± 0 | 27 ± 4 |