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. 2012 Jan;53(1):137–148. doi: 10.1194/jlr.M020065

TABLE 3.

Binding and biological activity parameters of CCK1R mutants

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.

a

P< 0.05 significantly different from wild-type CCK1R construct.

b

P< 0.05 significantly different from the same construct in the absence of MβCD treatment.

c

Values are expressed as number of sites/mg protein.