Synthetic Analogues of Huwentoxin-IV Spider Peptide With Altered Human Na_V1.7/Na_V1.6 Selectivity Ratios.

ABSTRACT: Huwentoxin-IV (HwTx-IV), a peptide discovered in the venom of the Chinese bird spider Cyriopagopus schmidti, has been reported to be a potent antinociceptive compound due to its action on the genetically-validated Na_V1.7 pain target. Using this peptide for antinociceptive applications in vivo suffers from one major drawback, namely its negative impact on the neuromuscular system. Although studied only recently, this effect appears to be due to an interaction between the peptide and the Na_V1.6 channel subtype located at the presynaptic level. The aim of this work was to investigate how HwTx-IV could be modified in order to alter the original human (h) Na_V1.7/Na_V1.6 selectivity ratio of 23. Nineteen HwTx-IV analogues were chemically s

SUBMITTER: Lopez L 

PROVIDER: S-EPMC8722715 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature