Table 3.
Effect of 4-substituted prolines on the affinity of peptidic inhibitor βMpCinn-Leu-Xaa-Apa
| # | Xaa | IC50 (nM)a | |
|---|---|---|---|
| 17 | Proline | Pro | 154 ± 10 |
| 19 | Sarcosine | Sar | 1540 ± 34 |
| 18 | cis-3,4-Methanoproline | mPro | 88 ± 11 |
| 20 | 4,4-Dimethylproline | 4,4-Me2Pro | 155 ± 31 |
| 21 | 4,4-Difluoroproline | 4,4-F2Pro | 121 ± 16 |
| 22 | cis-4-Fluoroproline | cis-4-FPro | 246 ± 62 |
| 23 | trans-4-Hydroxyproline | trans-4-HOPro | 166 ± 10 |
| 24 | cis-4-Hydroxyproline | cis-4-HOPro | 220 ± 27 |
| 25 | trans-4-Methoxyproline | trans-4-MeOPro | 317 ± 14 |
Affinity was determined by fluorescence polarization (Coleman et al. 2005)