Table 1

Agonist potency and basal activity at wild-type vs. mutant GLP-1Rs

All values represent the mean ± S.E.M. from four independent experiments.

ReceptorGLP-1Exendin-4Basal Activitya,b
EC50pEC50aEC50pEC50a
pMpM
hGLP-1R1.811.75 ± 0.041.311.90 ± 0.040.9 ± 0.2
P7L2.011.71 ± 0.061.411.87 ± 0.061.4 ± 0.5
R20K1.711.73 ± 0.071.111.95 ± 0.081.4 ± 0.5
R44H2.011.70 ± 0.071.611.79 ± 0.081.0 ± 0.3
R131Q1.811.74 ± 0.091.111.96 ± 0.081.4 ± 0.4
G168S1.611.79 ± 0.091.311.89 ± 0.091.1 ± 0.4
F260L2.211.65 ± 0.111.411.85 ± 0.121.3 ± 0.5
A316G2.011.58 ± 0.072.411.63 ± 0.630.9 ± 0.3
A316T2.611.70 ± 0.111.611.79 ± 0.101.4 ± 0.5
S333C2.211.66 ± 0.101.711.76 ± 0.101.2 ± 0.5
R421C2.611.58 ± 0.111.711.78 ± 0.091.1 ± 0.4

  • ↵a No significant difference vs. wild type.

  • ↵b Percentage of the corresponding GLP-1-induced maximum.