TABLE 2.
Affinity of mPPARα for nonfluorescent ligands determined by quenching of mPPARα aromatic amino acid fluorescence and by displacement of mPPARα-bound BODIPY C16-CoA
| Ligand | Chain Length: Double Bonds (Position) | Kd (nM) Fatty Acid | Kd (nM) Fatty Acyl-CoA | Ki (nM) Fatty Acid | Ki (nM) Fatty Acyl-CoA |
| Lauric acid/CoA | C12:0 | ND | ND | ND | ND |
| Palmitic acid/CoA | C16:0 | 92 ± 13 | 14 ± 2 | 135 ± 13 | 23 ± 4 |
| Palmitoleic acid/CoA | C16:1 (n-7) | 32 ± 3 | 24 ± 5 | 35 ± 3 | 31 ± 4 |
| Stearic acid/CoA | C18:0 | 81 ± 15 | 28 ± 5 | 134 ± 30 | 37 ± 5 |
| Oleic acid/CoA | C18:1 (n-9) | 22 ± 5 | 37 ± 5 | 37 ± 4 | 38 ± 6 |
| EPA/CoA | C20:5 (n-3) | 24 ± 6 | 17 ± 3 | 33 ± 5 | 21 ± 3 |
| DHA/CoA | C22:6 (n-3) | 31 ± 2 | 24 ± 2 | 34 ± 3 | 13 ± 3 |
| Clofibrate | 39 ± 6 | 46 ± 3 | |||
| Rosiglitazone | ND | ND |
Values represent the mean ± SE (n ≥ 3). ND, not determinable.