Ligand binding profile and free energy data for WT and K3.28A CB1
| Bmax | SR141716A | VCHSR | |||
|---|---|---|---|---|---|
| Kd | ΔG | Ki | ΔG | ||
| pmol/mg | nM | kJ/mol | nM | kJ/mol | |
| WT CB1 | 1.45 ± 0.41 | 2.3 ± 1.1 | −50.11 ± 1.20 | 31.3 ± 9.6 | −43.53 ± 0.77 |
| K3.28A | 1.61 ± 0.31 | 39.6 ± 10.51-150 | −42.94 ± 0.67 | 35.2 ± 1.4 | −43.24 ± 0.10 |
Saturation experiments using [3H]SR141716A were performed on stably transfected human embryonic kidney 293 cells to evaluate binding affinities and relative levels of receptor expression in the WT and mutant receptors. Inhibition constants were obtained from competition experiments using stably transfected human embryonic kidney293 cells. Data are the means ± S.E. of three independent experiments each performed in duplicate. ΔG values were calculated at 303°K using eq. 1. Statistics on free energy data were computed using propagation of error formula (Mortimer, 1981).
↵1-150 , statistically significant difference from WT (p < 0.05).