TABLE 1.
Binding affinities of LDL receptor interaction with intact and cleaved PCSK9
Kinetic constants were determined by biolayer interferometry using immobilized biotinylated LDL receptor ectodomain. Furin- and hepsin-cleaved PCSK9 (PCSK9c_fu and PCSK9c_hep) were purified by size exclusion chromatography using Ab-3D5. PCSK9 indicates intact PCSK9. The values are the averages ± S.D. of at least three independent experiments.
| Analyte | kon | koff | KD |
|---|---|---|---|
| 104m−1 s−1 | 10−4 s−1 | 10−9 m | |
| PCSK9 | 4.7 ± 1.0 | 61.2 ± 13.1 | 129.7 ± 17.4 |
| PCSK9c_hep | 3.2 ± 0.6 | 85.8 ± 18.0 | 267.7 ± 10.9 |
| PCSK9 | 3.6 ± 0.5 | 62.4 ± 12.4 | 177.0 ± 38.9 |
| PCSK9c_fu | 3.9 ± 0.5 | 138.5 ± 2.7 | 356.5 ± 50.7 |