Table 2. EC50 values of D-amino acid substituted and Asn1 substituted/modified peptides for GALR2 and GALR3.
Substitution/Modification | GALR2 |
GALR3 |
||
---|---|---|---|---|
EC50(nM) | Emax(Fold induction) | EC50(nM) | Emax(Fold induction) | |
dN1 | 21.38 ± 5.54 | 15.22 | 38.90 ± 8.00 | 36.80 |
dW2 | 100.00 ± 18.71 | 16.94 | 138.04 ± 23.22 | 33.01 |
dT3 | NM | NM | NM | NM |
dA4 | 97.72 ± 18.29 | 16.5 | 112.20 ± 23.07 | 27.51 |
dA6 | 208.93 ± 26.96a | 17.14 | 316.23 ± 47.07a | 31.76 |
dY9 | NM | NM | NM | NM |
dL10 | NM | NM | NM | NM |
dA12 | 1230.26 ± 158.75a | 17.19 | 1412.54 ± 210.27a | 37.2 |
dQa14 | 77.62 ± 15.97 | 15.89 | 323.59 ± 66.55a | 33.88 |
pQ1 | 35.01 ± 7.82 | 15.85 | 61.66 ± 10.37 | 33.08 |
Ac-N1 | 58.88 ± 11.02 | 16.73 | 81.28 ± 16.71 | 31.01 |
PEG-N1 | 61.65 ± 16.99 | 14.99 | 173.78 ± 25.87 | 31.39 |
Cit1 | 61.66 ± 19.00 | 16.26 | 251.19 ± 64.98 | 30.40 |
Fmoc | 77.62 ± 15.97 | 15.24 | 125.89 ± 25.89 | 31.77 |
aP < 0.05 vs. WT SPX, NM, Not Measurable.