Table 1. Overview of effects of glucagon-like peptide-1 receptor (GLP-1R) V229A in inactive and active states compared with GLP-1R wild-type (WT).
(↑ increased, ↓ decreased, ≈ unchanged).
| Assay | GLP-1R V229A vs GLP-1R WT | |
|---|---|---|
| Vehicle (inactive) | Exendin-4 (active) | |
| Surface expression | ≈ (↓) | N/A |
| Cholesterol binding | ↓ | ≈ |
| Plasma membrane diffusion | ↓↓ | ≈ |
| Plasma membrane displacement | ↓ | ≈ |
| Plasma membrane speed | ↓ | ≈ |
| Oligomerisation | ↑ | ≈ |
| Lipid raft recruitment | ↑ | ↑ |
| CCP recruitment | ≈ | ↓ |
| Internalisation | N/A | ↓ |
| Recycling | N/A | ↑ |
| Degradation | N/A | ≈ |
| Mini-Gs recruitment | N/A | ↑↑ |
| β-arrestin 2 recruitment | N/A | ↑ |
| Mini-Gq recruitment | N/A | ≈ |
| Activation at plasma membrane | N/A | ↑↑ |
| Activation at endosomes | N/A | ↑ |
| cAMP | N/A | ↑ |
| Insulin secretion | ↓ cells / ≈ islets | ≈ cells / ↑ islets |