Table 2.
Summary of potent HNTX-III analogues
| ID | Peptide | Amino acid sequence | hNav1.7 IC50 (μM) |
|---|---|---|---|
| 1 | Native HNTX-III | GCKGF GDSCT PGKNE CCPNY ACSSK HKWCK VYL | 0.211 ± 0.049 |
| 37 | A21L-V | GCKGF GDSCT PGKNE CCPNY LVCSSK HKWCK VYL | 0.047 ± 0.016 |
| 38 (H0) | K0G1-P18K-A21V | KGCKGF GDSCT PGKNE CCKNY VCSSK HKWCK VYL | 0.040 ± 0.006 |
| 39 (H1) | K0G1-A21L-V | KGCKGF GDSCT PGKNE CCPNY LVCSSK HKWCK VYL | 0.027 ± 0.007 |
| 40 (H2) | P18K-A21L-V | GCKGF GDSCT PGKNE CCKNY LVCSSK HKWCK VYL | 0.013 ± 0.002 |
| 41 (H3) | K0G1-N19L-A21L-V | KGCKGF GDSCT PGKNE CCPLY LVCSSK HKWCK VYL | 0.017 ± 0.005 |
| 42 (H4) | K0G1-P18K-A21L-V | KGCKGF GDSCT PGKNE CCKNY LVCSSK HKWCK VYL | 0.007 ± 0.001 |
| 43 (H5) | K0G1-P18K-A21V-V | KGCKGF GDSCT PGKNE CCKNY VVCSSK HKWCK VYL | 0.526 ± 0.048 |
| 44 (H6) | K0G1-P18K-A21L-L | KGCKGF GDSCT PGKNE CCKNY LLCSSK HKWCK VYL | 0.087 ± 0.017 |
| 45 (H7) | K0G1-N19L-A21L-L | KGCKGF GDSCT PGKNE CCPLY LLCSSK HKWCK VYL | 0.121 ± 0.010 |
| 46 (H8) | K0K1-P18K-A21L-L | KKCKGF GDSCT PGKNE CCKLY LLCSSK HKWCK VYL | 0.112 ± 0.027 |
| 47 (H9) | K0K1-N19L-A21L-L | KKCKGF GDSCT PGKNE CCPLY LLCSSK HKWCK VYL | 0.048 ± 0.022 |
| 48 (H10) | K0L1-P18K-A21L-L | KLCKGF GDSCT PGKNE CCKNY LLCSSK HKWCK VYL | 0.022 ± 0.003 |
The amino acid residues in bold represent mutated residues in the amino acid sequence. Data are shown mean ± SD, n = 3 to 5 cells, one-way ANOVA followed by Dunnett’s post hoc tests.