TABLE 1.
Screening data for mutant cycle analysis. Peptide inhibition of wild-type or α subunit mutant ENaC was determined at the indicated [peptide]. Mutant channel inhibition is expressed relative to wild-type channel inhibition for the same peptide. Values are expressed as mean (n = 2–3).
Inhibition |
|||||||
---|---|---|---|---|---|---|---|
LPHPLQRL (10 μm) | APHPLQRL (30 μm) | LGHGLQRL (50 μm) | LPKPLQRL (50 μm) | LPHPLARL (10 μm) | LPHPLQAL (10 μm) | LPHPLQRA (50 μm) | |
% | |||||||
Wild-type | 77.22 | 52.19 | 51.22 | 42.24 | 51.22 | 49.64 | 41.82 |
Inhmut/Inhwild type | |||||||
G252W | 0.15 | 0.14 | 0.23 | 0.37 | |||
Q254W | 0.39 | 0.34 | 0.30 | 0.70 | |||
L255W | 0.46 | 0.20 | 0.14 | 0.21 | 0.19 | ||
C256W | 0.49 | 0.40 | 0.25 | 0.17 | 0.50 | ||
T267W | 0.11 | 0.13 | −0.02 | 0.11 | 0.02 | ||
A274W | 0.52 | 0.41 | 0.56 | 0.52 | 0.37 | 0.36 | 0.31 |
V275W | 0.43 | 0.35 | 0.41 | 0.31 | 0.21 | 0.23 | 0.18 |
R289W | 0.29 | 0.21 | 0.32 | 0.48 | 0.20 | 0.20 | 0.11 |
D473W | 0.76 | 0.73 | 0.67 | 1.02 | 0.54 | 0.48 | 0.48 |