Table 1. Peptide sequences synthesized and their potency in activity assays with FRET1 and insulin.
Name | N-term | Sequence | C-term | Ki FRET1 (μM) | Ki Insulin (μM) |
---|---|---|---|---|---|
C7C-1 | NH3+ | ACSWWSIHLCG | COO- | 112 ± 6 | 3.7 ± 0.7 |
C7C-1A | NH3+ | ACSWWSIHLCG | amide | >100 | >10 |
C7C-1B | NH3+ | ACSWWSIHLCGGG | COO- | >100 | >10 |
C7C-2 | NH3+ | ACNAGHLSQCG | COO- | >500 | >10 |
C7C-2A | NH3+ | ACNAGHLSQCG | amide | >500 | >10 |
P12-1 | NH3+ | VHWDFRQWWQPS | COO- | 7.7 ± 0.7 | 0.8 ± 0.04 |
P12-1A | NH3+ | VHWDFRQWWQPS | amide | 5.0 ± 0.3 | 1.3 ± 0.2 |
P12-1B | NH3+ | VHWDFRQW | amide | 41 ± 6.4 | 7.0 ± 1.7 |
P12-1C | acetyl | FRQWWQPS | COO- | 139 ± 21 | >10 |
P12-1D | acetyl | WDFRQWWQ | amide | 140 ± 28 | >10 |
P12-2 | NH3+ | LNFPMPSRPHSS | COO- | >100 | >10 |
P12-2A | NH3+ | LNFPMPSRPHSS | amide | >100 | >10 |
P12-2B | NH3+ | LNFPMPSR | amide | >500 | >10 |
P12-2C | acetyl | MPSRPHSS | COO- | >500 | >10 |
P12-2D | acetyl | FPMPSRPH | amide | >500 | >10 |
P12-3 | NH3+ | QSLPWCYPHCVT | COO- | 8.9 ± 0.3 | 3.9 ± 1.6 |
P12-3A | NH3+ | QSLPWCYPHCVT | amide | 10 ± 0.4 | 4.1 ± 0.3 |
P12-3B | NH3+ | QSLPWCYP | amide | 39 ± 20 | >10 |
P12-3C | acetyl | WCYPHCVT | COO- | 35 ± 4.7 | >10 |
P12-3D | acetyl | LPWCTPHC | amide | 102 ± 14 | >10 |
P12-4 | NH3+ | WSPISGKFFQRF | COO- | 3.9 ± 0.5 | 1.5 ± 0.3 |
P12-4A | NH3+ | WSPISGKFFQRF | amide | 4.2 ± 1.3 | 2.6 ± 0.7 |
P12-4B | NH3+ | WSPISGKF | amide | >500 | >10 |
P12-4C | acetyl | SGKFFQRF | COO- | >500 | >10 |
P12-4D | acetyl | PISGKFFQ | amide | >500 | >10 |