Table 2.
Allosteric parameters for WT and G252A, L256A, V259A GLP-1Rs
| GLP-1R wild type |
GLP-1R(G252A, L256A, V259A) |
|||
| Interacting ligands | pKB | Logαβ (αβ) | pKB | Logαβ (αβ) |
| Compound 2 | 5.56 ± 0.13 | 4.71 ± 0.21 | ||
| GLP-1(7-36)NH2 | 0.59 ± 0.11 (3.9) | 0.13 ± 0.15 (1.3) | ||
| Oxyntomodulin | 1.46 ± 0.15 (29) | 1.74 ± 0.12 (55) | ||
| BETP | 5.20 ± 0.20 | 4.78 ± 0.15 | ||
| Oxyntomodulin | 1.14 ± 0.14 (14) | 1.62 ± 0.11 (42) | ||
Quantitative parameters for the allosteric interaction of compound 2 or BETP with GLP-1(7-36)NH2 or oxyntomodulin. cAMP data were analyzed with an operational model of allosterism as defined in Methods. pKB values represent the negative logarithm of the affinity for the allosteric ligands derived from application of the operational model of allosterism. Logαβ values represent the composite cooperativity between the allosteric modulator and the orthosteric ligand. Antilogarithms are shown in parentheses.