TABLE 3.
Constructs | Binding Affinities | Binding Sites | Calcium Responses | |||
Ki | Sites/cell × 105 | EC50 | ||||
nM | nM | |||||
Untreated | + MβCD | Untreated | +MβCD | Untreated | +MβCD | |
CCK1R, WT | 4.3 ± 1.0 | 58.7 ± 10.5b | 3.4 ± 0.5 | 2.1 ± 0.3 | 0.05 ± 0.01 | 0.24 ± 0.03b |
CCK1R(Y140A) | 0.6 ± 0.1a | 0.8 ± 0.2 | 3.3 ± 0.6 | 2.3 ± 0.9 | 0.40 ± 0.08a | 0.42 ± 0.11 |
CCK1R(W166A) | 9.6 ± 2.4a | 7.4 ± 1.5 | 2.6 ± 0.4c | 3.0 ± 0.7c | 0.29 ± 0.06a | 0.50 ± 0.09b |
CCK1R(Y237A) | 37.5 ± 3.8a | 65.9 ± 5.1b | 3.8 ± 0.3 | 3.2 ± 0.2 | 0.05 ± 0.02 | 0.32 ± 0.07b |
Data are expressed as means ± SEM of values from three to seven independent experiments.
P< 0.05 significantly different from wild-type CCK1R construct.
P< 0.05 significantly different from the same construct in the absence of MβCD treatment.
Values are expressed as number of sites/mg protein.