WT- CCK2R | Y189F Mutant | N358A Mutant | ||||
---|---|---|---|---|---|---|
Ki | FCCK-9 | Ki | FCCK-9 | Ki | FCCK-9 | |
nM | nM | nM | ||||
CCK-9 | 1.3 ± 0.3 | 1 | 39.3 ± 5.6 | 1 | 24.2 ± 5.3 | 1 |
(PheCH3)9-CCK | 17.4 ± 3.2 | 13 | 252 ± 42 | 6 | 26.1 ± 7.8 | 1 |
(Phenylethylamide)9-CCK | 341 ± 53 | 262 | 816 ± 157 | 21 | 543 ± 154 | 22 |
(Ala)3-CCK | 18.1 ± 6.1 | 14 | 382 ± 15 | 10 | 233 ± 55 | 10 |
Ki values were calculated from competition curves of 125I-BH-CCK-9 binding by the indicated ligand as described under Materials and Methods. The factor FCCK-9 represents the effect of the mutation on the affinity of the ligand tested relative to CCK-9. Results are expressed as mean ± S.E. of three to five separate experiments performed in duplicate.