Modulation of Kv2.1 channel gating and TEA sensitivity by distinct domains of SNAP-25

Biochem J. 2006 Jun 1;396(2):363-9. doi: 10.1042/BJ20051478.

Abstract

Distinct domains within the SNARE (soluble N-ethylmaleimide-sensitive fusion protein attachment protein receptor) proteins, STX1A (syntaxin 1A) and SNAP-25 (synaptosome-associated protein-25 kDa), regulate hormone secretion by their actions on the cell's exocytotic machinery, as well as voltage-gated Ca2+ and K+ channels. We examined the action of distinct domains within SNAP-25 on Kv2.1 (voltage gated K+ 2.1) channel gating. Dialysis of N-terminal SNAP-25 domains, S197 (SNAP-25(1-197)) and S180 (SNAP-25(1-180)), but not S206 (full-length SNAP-25(1-206)) increased the rate of Kv2.1 channel activation and slowed channel inactivation. Remarkably, these N-terminal SNAP-25 domains, acting on the Kv2.1 cytoplasmic N-terminus, potentiated the external TEA (tetraethylammonium)-mediated block of Kv2.1. To further examine whether these are effects of the channel pore domain, internal K+ was replaced with Na+ and external K+ was decreased from 4 to 1 mM, which decreased the IC50 of the TEA block from 6.8+/-0.9 mM to >100 mM. Under these conditions S180 completely restored TEA sensitivity (7.9+/-1.5 mM). SNAP-25 C-terminal domains, SNAP-25(198-206) and SNAP-25(181-197), had no effect on Kv2.1 gating kinetics. We conclude that different domains within SNAP-25 can form distinct complexes with Kv2.1 to execute a fine allosteric regulation of channel gating and the architecture of the outer pore structure in order to modulate cell excitability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation
  • Animals
  • Anti-Dyskinesia Agents / metabolism
  • Anti-Dyskinesia Agents / pharmacology
  • Botulinum Toxins / metabolism
  • Botulinum Toxins / pharmacology
  • Botulinum Toxins, Type A / metabolism
  • Botulinum Toxins, Type A / pharmacology
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Electrophysiology
  • Humans
  • Ion Channel Gating* / drug effects
  • Peptides / metabolism
  • Protein Binding
  • Protein Structure, Tertiary*
  • Rats
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Sensitivity and Specificity
  • Shab Potassium Channels / genetics
  • Shab Potassium Channels / metabolism*
  • Synaptosomal-Associated Protein 25 / genetics
  • Synaptosomal-Associated Protein 25 / metabolism*
  • Synaptosomal-Associated Protein 25 / pharmacology
  • Tetraethylammonium / metabolism
  • Tetraethylammonium / pharmacology*
  • Transfection

Substances

  • Anti-Dyskinesia Agents
  • Kcnb1 protein, rat
  • Peptides
  • Recombinant Fusion Proteins
  • Shab Potassium Channels
  • Snap25 protein, rat
  • Synaptosomal-Associated Protein 25
  • Tetraethylammonium
  • Botulinum Toxins
  • Botulinum Toxins, Type A
  • botulinum toxin type E