A centipede toxin causes rapid desensitization of nociceptor TRPV1 ion channel

Aiqin Zhu, Aerziguli Aierken, Zhihao Yao, Simon Vu, Yuhua Tian, Jie Zheng, Shilong Yang, Fan Yang

Research output: Contribution to journalArticle

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Abstract

The nociceptive transient receptor potential vanilloid 1 (TRPV1) ion channel is a polymodal receptor for multiple painful stimuli, hence actively pursued as a target for analgesic drugs. We identified a small peptide toxin RhTx2 from the Chinese red-headed centipede that strongly modulates TRPV1 activities. RhTx2, a 31-amino-acid peptide, is similar to a TRPV1-activating toxin RhTx we have previously discovered but with four extra amino acids at the N terminus. We observed that, like RhTx, RhTx2 activated TRPV1, but RhTx2 rapidly desensitized the channel upon prolonged exposure. Desensitization was achieved by reducing both the open probability and the single-channel conductance. RhTx2 is not only a tool to study the desensitization mechanism of TRPV1, but also a promising starting molecule for developing novel analgesics.

Original languageEnglish (US)
Pages (from-to)41-49
Number of pages9
JournalToxicon
Volume178
DOIs
StatePublished - Apr 30 2020

Keywords

  • Desensitization
  • Gating mechanisms
  • Nociception
  • Peptide toxins
  • TRPV1

ASJC Scopus subject areas

  • Toxicology

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    Zhu, A., Aierken, A., Yao, Z., Vu, S., Tian, Y., Zheng, J., Yang, S., & Yang, F. (2020). A centipede toxin causes rapid desensitization of nociceptor TRPV1 ion channel. Toxicon, 178, 41-49. https://doi.org/10.1016/j.toxicon.2020.02.016