Table 2.
Efficacy and potency of OEA on wild-type GPR119 and receptor mutants as well as the potency fold change between wild type and mutants (Fmut)
| Mutant | Emax | OEA EC50 | Fmut | n | |||
|---|---|---|---|---|---|---|---|
| (%) | SEM | Log | SEM | nM | |||
| Wild type | 97 | 2.0 | −6.54 | 0.13 | 290 | 7 | |
| Binding pocket | |||||||
| GlnII:24Ala (65) | 101 | 5.6 | −6.23 | 0.26 | 596 | 3.5 | 3 |
| ArgIII:04Ala (81) | 34* | 2.4 | −5.83 | 0.12 | 1470 | 8.6 | 3 |
| MetIII:05Ala (82) | 26* | 1.5 | −6.01 | 0.08 | 975 | 5.7 | 3 |
| ValIII:08Ala (85) | 97 | 3.4 | −6.18 | 0.12 | 663 | 3.9 | 3 |
| ThrIII:09Ala (86) | 37* | 2.1 | −6.11 | 0.20 | 784 | 2.0 | 4 |
| ThrIII:09Val (86) | 63* | 8.7 | −6.59 | 0.77 | 257 | 0.67 | 4 |
| AlaIII:12Val (89) | 116 | 19.0 | −5.80 | 0.42 | 1600 | 4.1 | 4 |
| ValV:05Ala (166) | 69 | 13.0 | −6.07 | 0.88 | 861 | 2.2 | 3 |
| SerV:09Ala (170) | 120 | 16.0 | −6.73 | 0.65 | 185 | 0.5 | 4 |
| SerV:09Val (170) | 47* | 17.0 | −5.76 | 0.70 | 1760 | 4.6 | 4 |
| TrpVI:13Ala (238) | – | – | – | – | – | – | 3 |
| PheVI:16Ala (241) | – | – | – | – | – | – | 3 |
| GlyVI:20Val (245) | 80 | 2.6 | −6.58 | 0.28 | 262 | 1.5 | 3 |
| GlnVI:23Ala (248) | 73 | 8.4 | −5.90 | 0.39 | 1270 | 3.3 | 3 |
| GluVII:02Ala (261) | 71 | 9.2 | −5.69 | 0.28 | 2040 | 12.0 | 3 |
| ArgVII:03Ala (262) | 20* | 2.7 | −5.54 | 0.17 | 2860 | 17.0 | 3 |
| TrpVII:06Ala (265) | – | – | – | – | – | – | 4 |
| GlyVII:09Val (268) | 43* | 2.5 | −5.79 | 0.30 | 1630 | 9.6 | 3 |
| ECL-2b | |||||||
| PheC+2Ala (157) | – | – | – | – | – | – | 3 |
| PheC+3Ala (158) | 19* | 2.9 | –5.12 | 0.51 | 7816 | 21.0 | 4 |
Statistically significant changes from wild type are marked with an asterisk
(*).
Residue positions are given in parentheses after the Schwartz/Baldwin name.