Structural determinants for alpha-neurotoxin sensitivity in muscle nAChR and their implications for the gating mechanism

Channels (Austin). 2007 Jul-Aug;1(4):234-7. doi: 10.4161/chan.4909. Epub 2007 Aug 20.

Abstract

Neurotoxins from snake venoms act as potent antagonists on the nicotinic acetylcholine receptors (nAChRs). Alpha-neurotoxins such as alpha-bungarotoxin (alpha-Btx) selectively bind to the skeletal muscle nAChRs among other subtypes, causing failure of the neuromuscular transmission. Through evolution, some species including snakes and mongoose have developed resistance to alpha-neurotoxins via specific amino acid substitutions in their muscle-type nAChR alpha1 subunit, which constitutes most of the toxin-binding site. Here we analyze these sequence variations in the context of our recent crystal structure of the extracellular domain of the mouse nAChR alpha1 bound to alpha-Btx. Our structure suggests that alpha-Btx has evolved as an extremely potent antagonist of muscle nAChR by binding the receptor tightly, blocking its ligand site, and locking its conformation in a closed state. Conversely, most toxin-resistant mutations occur at the alpha-Btx binding interface on nAChR alpha1 but away from the agonist binding site. These mutations can interfere with the binding of alpha-Btx without having deleterious effect on the gating function. These analyses not only help understand the structural determinants for neurotoxin sensitivity in muscle-type nAChR, but also shed light on its gating mechanism.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Bungarotoxins / metabolism
  • Bungarotoxins / pharmacology*
  • Drug Resistance
  • Evolution, Molecular
  • Humans
  • Ion Channel Gating / drug effects*
  • Ligands
  • Models, Molecular
  • Molecular Sequence Data
  • Muscle, Skeletal / drug effects*
  • Muscle, Skeletal / metabolism
  • Mutation
  • Neuromuscular Junction / drug effects
  • Neuromuscular Junction / metabolism
  • Neurotoxins / metabolism
  • Neurotoxins / pharmacology*
  • Nicotinic Antagonists / metabolism
  • Nicotinic Antagonists / pharmacology*
  • Protein Binding
  • Protein Conformation
  • Protein Subunits
  • Receptors, Nicotinic / chemistry
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / genetics
  • Receptors, Nicotinic / metabolism
  • Structure-Activity Relationship
  • Synaptic Transmission / drug effects

Substances

  • Bungarotoxins
  • Ligands
  • Neurotoxins
  • Nicotinic Antagonists
  • Protein Subunits
  • Receptors, Nicotinic