Design, synthesis, and mechanism of action of novel μ-conotoxin KIIIA analogues for inhibition of the voltage-gated sodium channel Nav1.7

Keywords

μ-conotoxin

voltage-gated sodium ion channel

analgesia

structure optimization

peptide synthesis

KIIIA

AbbreviationsDab

L-2,4-diaminobutyric acid

Dapa

L-2,3-diaminopropionic acid

DIPEA

N,N′-diisopropylethylamine

Fmoc

9-fluorenylmethoxycarbonyl

HCTU

5-chloro-1-[bis(dimethylamino)methylene]-1H-benzotriazolium 3-oxide hexafluorophosphate

Nav

voltage-gated sodium channel

RP-HPLC

reversed-phase high-performance liquid chromatography

TTX-r

Tetrodotoxin-resistant

© 2023 THE AUTHORS. Published by Elsevier Inc on behalf of American Society for Biochemistry and Molecular Biology.

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