A 4/8 Subtype α-Conotoxin Vt1.27 Inhibits N-Type Calcium Channels With Potent Anti-Allodynic Effect.

ABSTRACT: A novel 4/8 subtype α-conotoxin, Vt1.27 (NCCMFHTCPIDYSRFNC-NH₂), was identified from Conus vitulinus in the South China Sea by RACE methods. The peptide was synthesized and structurally characterized. Similar to other α-conotoxins that target neuronal nicotinic acetylcholine receptor (nAChR) subtypes, Vt1.27 inhibited the rat α3β2 nAChR subtype (IC₅₀ = 1160 nM) and was inactive at voltage-gated sodium and potassium channels in rat sensory neurons. However, Vt1.27 inhibited high voltage-activated N-type (Ca_V2.2) calcium channels expressed in HEK293T cells with an IC₅₀ of 398 nM. An alanine scan of the peptide showed that residues Phe⁵, Pro⁹, Ile¹⁰, and Ser¹³ contribute significantly to the inhibit

SUBMITTER: Wang S 

PROVIDER: S-EPMC9230573 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature