Table 2.
SPR binding data and kinetic parameters for peptides monitored over BACE1 and BACE2 protein surfaces.
| Peptide | Protein | kon (1/Ms) | koff (1/s) | KD (M) | Selectivity for BACE1b |
|---|---|---|---|---|---|
| Exo-Pep#6 | BACE1 | 2.5·10− 5 | |||
| BACE2 | 6.6·10− 5 | ||||
| Active-Pep#1 | BACE1 | 2.5–4.0·103 | < 1·10− 6 | < 1·10− 9 | |
| BACE2 | 2.7–3.1·103 | 7.8–8.3·10− 4 | 2.5–3.1·10− 7 | > 280 | |
| Active-exo-Pep#12 | BACE1 | 1.1–1.3·105 | < 1·10− 6 | < 1·10− 11 | |
| BACE1 | 1.1–1-3·105 | 1.2–2.5·10− 5 | 1.1–2.0·10− 10 | > 15a |
a
As slow dissociation rate constant (koff) monitored for this interaction is on the limit of the instrument resolution the effective affinity and thus selectivity might be significantly higher.
b
Selectivity for BACE1 calculated as ratio KD(BACE2)/KD(BACE1).