Synthesis of an acetylcholine receptor-specific toxin derivative regioselectively labeled with an undecagold cluster

Bioconjug Chem. 1994 May-Jun;5(3):199-204. doi: 10.1021/bc00027a004.

Abstract

The regioselective modification of a snake curaremimetic toxin is described. Toxin-alpha from Naja nigricollis was derivatized with an electron-dense maleimido undecagold cluster 5. The cluster-bound obtained toxin 8 has a very high affinity for the cholinergic binding site (Ki = 70 pM) of Torpedo marmorata nicotinic receptor. It is harboring a compact heavy atom core of about 8 A which makes it very useful for electron microscopy experiments.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Cobra Neurotoxin Proteins / chemical synthesis*
  • Cobra Neurotoxin Proteins / chemistry
  • Cobra Neurotoxin Proteins / metabolism
  • In Vitro Techniques
  • Molecular Structure
  • Nicotinic Antagonists*
  • Organogold Compounds
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / metabolism
  • Receptors, Nicotinic / metabolism
  • Torpedo / metabolism

Substances

  • Cobra Neurotoxin Proteins
  • Nicotinic Antagonists
  • Organogold Compounds
  • Organometallic Compounds
  • Receptors, Nicotinic
  • undecagold
  • alpha-cobratoxin