Table 1

Affinities of CCK-9 and modified peptides for the WT-CCK2R, Y189F (Y4.60F) mutant, and N358A (N6.55A) mutant

WT- CCK2RY189F MutantN358A Mutant
KiFCCK-9KiFCCK-9KiFCCK-9
nM nM nM
CCK-91.3  ± 0.3139.3  ± 5.6124.2  ± 5.31
(PheCH3)9-CCK17.4  ± 3.213252  ± 42626.1  ± 7.81
(Phenylethylamide)9-CCK341  ± 53262816  ± 15721543  ± 15422
(Ala)3-CCK18.1  ± 6.114382  ± 1510233  ± 5510

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.