Poster Presentation 11th Asia-Pacific Congress of the International Society on Toxinology 2021

A novel spider toxin inhibits the fast inactivation of Nav1.9 channel by binding to the domain III and domain IV voltage-sensors (#106)

Shuijiao Peng 1 , minzhi chen 1 , Zhen Xiao 1 , Xin Xiao 1 , Sen Luo 1 , Songping Liang 1 , Xi Zhou 1 , Zhonghua Liu 1
  1. The National and Local Joint Engineering Laboratory of Animal Peptide Drug Development, College of Life Sciences, Hunan Normal University, Changsha, China

Venomous animals have evolved to produce peptide toxins that modulate the activity of voltage-gated sodium (Nav) channels. These specific modulators are powerful probes to investigate the structural and functional features of Nav channels. Here, we isolated and characterized δ-theraphotoxin-Gr4b (Gr4b), a novel peptide toxin from the venom of the spider Grammostola rosea. Gr4b contains 37-amino acid residues with six cysteines forming three disulfide bonds. Moreover, Patch-clamp analysis confirmed that Gr4b markedly slows the fast inactivation of Nav1.9, and it also inhibits the currents of Nav1.3-Nav1.7, but it does not affect Nav1.8. Gr4b significantly shifts the steady-state activation and inactivation curves of Nav1.9 to the depolarization direction, and increases the window current, which is consistent with the change of the ramp current. Furthermore, analysis of Nav1.9/Nav1.8 chimeric channel revealed that Gr4b preferentially binds to the domain III voltage-sensor (DIII VSD) and has additional interactions with the DIV VSD. The alanine-screening analysis indicated that N1139 and L1143 in DIII s3-s4 linker participate in toxin binding. Taken together, our study reported a novel spider peptide toxin that slows the fast inactivation of Nav1.9 by binding to a new neurotoxin receptor site-DIII VSD. These findings provide insight into a functional role of Nav channel DIII VSD in fast inactivation.