Efficacy, potency, and helicity of distinct apoE peptides for α7 nAChR inhibition
Data represent the mean ± S.E.M. of five to 15 oocytes per peptide. IC50 values are presented with 95% confidence intervals. Percentage of helicity was measured in the presence of 40% TFE (see Materials and Methods).
Peptide | Maximal Inhibition (3 μM) | IC50 | Helicity |
|---|---|---|---|
| μM | % | ||
| ApoE133-149 | 91 ± 3 | 0.45 (0.35-0.57) | 46.5 |
| ApoE133-140 | 16 ± 3 | 2.6 | |
| ApoE141-148 | 85 ± 1 | 1.3 (1.1-1.6) | 12.8 |
| ApoE144-148 | 25 ± 4 | ||
| RLKKLRLR | 35 ± 4 | 4.5 | |
| KKLLLRRR | 23 ± 4 | 6.5 | |
| KKKKK | 10 ± 2 | ||
| LRVRLASH- | 93 ± 7 | 0.62 (0.38-1.0) | N.D. |
| LRLLRLRLL | |||
| LRLLRLRL | 74 ± 8 | 2.2 (0.44-10) | N.D. |
| LRELRERL | 2 ± 1 | 37.4 | |
| LLKLRKLL | 7 ± 2 |
| N.D. |
N.D., not determined because of suspension in dimethyl sulfoxide.