Hydroxy acid mutations to putative backbone hydrogen bonding groups of the binding site’s complementary face
EC50 values (μM) reported. Full data, including error estimates, are reported in Supplemental Table 2.
| Acetylcholine | Epibatidine | Varenicline | |
|---|---|---|---|
| Probing Leu119 NH | |||
| wt recovery (Leu)a | 120 | 0.29 | 2.3 |
| Mutant (Lah) | 180 | 0.75 | 3.2 |
| Fold shift | 1.5 | 2.6 | 1.4 |
| Probing Asn107 CO | |||
| wt recovery (Val)a | 100 | 0.40 | 2.3 |
| Mutant (Vah) | 180 | 0.64 | 10 |
| Fold shift | 1.8 | 1.6 | 4.3 |
Lah, α-hydroxyleucine; Vah, α-hydroxyvaline; wt, wild-type.
↵a Expression of the wild-type receptor with the natural amino acid incorporated by nonsense suppression.