Table 4.
Selectivity factors calculated for 5 fluorogenic substrates containing unnatural amino acids designed based on HyCoSuL profiling. Substrates that discriminate between caspases by factors lower than 40-fold are bolded.
| Substrate | Target | Selectivity factor (kcat/KM casp-of interest : kcat/KM casp-X)
|
|||||
|---|---|---|---|---|---|---|---|
| → Casp-3 | → Casp-6 | → Casp-7 | → Casp-8 | → Casp-9 | → Casp-10 | ||
| MPP39 15 | Casp-3 | - | 5000 | 4.5 | 120 | > 10000 | 600 |
| Casp-7 | 0.22 | 1125 | - | 27 | 2500 | 135 | |
|
| |||||||
| MPP36 16 | Casp-6 | 19.8 | - | 47.5 | 45.1 | > 10000 | 4.6 |
|
| |||||||
| MPP30 17 | Casp-8 | 65.5 | 980 | 150 | - | 73 | 53 |
|
| |||||||
| MPP8 18 | Casp-9 | > 10000 | 1070 | > 10000 | 12.4 | - | 33.5 |
|
| |||||||
| MPP52 19 | Casp-10 | 147 | 515 | 286 | 79 | 32 | - |