Table 4. Receptor-binding affinity of cyclosporins to FPR1 haplotypes.
| fNLFNYK–FITC-binding parameters* | pKi for cyclosporins† | |||
|---|---|---|---|---|
| Haplotype | Kd (nM) | Bmax | pKi for CsA | pKi for CsH |
| CH1 | 2.0±0.2 | 48336±4553 | 7.15±0.05 | 8.16±0.16 |
| CH2 | 1.7±0.1 | 47657±9098 | 5.26±0.02‡ | 6.34±0.04‡ |
| CH3 | 1.8±0.2 | 59135±4185 | 5.62±0.09‡ | 6.48±0.04‡ |
| CH4 | 1.3±0.2‡ | 33860±4977 | 5.99±0.12‡ | 6.16±0.08‡ |
| CH5 | 2.8±0.1‡ | 42575±4902 | 6.86±0.08 | 7.75±0.09 |
| CH6 | 1.8±0.4 | 34093±693 | 5.63±0.02‡ | 6.46±0.05‡ |
| CH7 | 1.7±0.3 | 60688±10388 | 5.85±0.02‡ | 6.47±0.04‡ |
| CH8 | 1.3±0.1‡ | 36362±353 | 6.96±0.11 | 7.90±0.08 |
| CH9 | 1.9±0.5 | 39009±6672 | 7.05±0.09 | 7.91±0.11 |
| CH10 | 2.4±0.3 | 41751±615 | 7.13±0.12 | 7.94±0.06 |
| CH11 | 2.2±0.7 | 37713±5841 | 5.59±0.01‡ | 6.27±0.02‡ |
| CH12 | 3.2±0.3‡ | 65059±3570 | 7.26±0.02 | 7.91±0.01 |
*CHO-Gα16 cells stably transfected with individual variants of FPR1 (CH1–CH12) were incubated with various concentrations of fNLFNYK–FITC. The data were analysed by non-linear least-squares analysis to determine Kd and Bmax values.
†Cells were incubated with various concentrations of cyclosporins together with 1 nM fNLFNYK–FITC. Ki was determined by non-linear least-squares analysis using the known Kd for fNLFNYK–FITC and the observed IC50 of cyclosporins for different FPR1 variants.
‡P<0.05 compared with CH1.