Revealing the molecular determinants of neurotoxin specificity for calcium-activated versus voltage-dependent potassium channels

Biochemistry. 2007 May 8;46(18):5358-64. doi: 10.1021/bi700150t. Epub 2007 Apr 18.

Abstract

Potassium channel dysfunction underlies diseases such as epilepsy, hypertension, cardiac arrhythmias, and multiple sclerosis. Neurotoxins that selectively inhibit potassium channels, alpha-KTx, have provided invaluable information for dissecting the contribution of different potassium channels to neurotransmission, vasoconstriction, and lymphocyte proliferation. Thus, alpha-KTx specificity comprises an important first step in potassium channel-directed drug discovery for these diseases. Despite extensive functional and structural studies of alpha-KTx-potassium channel complexes, none have predicted the molecular basis of alpha-KTx specificity. Here we show that by minimizing the differences in binding free energy between selective and nonselective alpha-KTx we are able to identify all of the determinants of alpha-KTx specificity for calcium-activated versus voltage-dependent potassium channels. Because these determinants correspond to unique features of the two types of channels, they provide a way to develop more accurate models of alpha-KTx-potassium channel complexes that can be used to design novel selective alpha-KTx inhibitors.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence
  • Amino Acid Substitution / genetics
  • Animals
  • CHO Cells
  • Cell Line
  • Charybdotoxin / chemistry
  • Charybdotoxin / genetics
  • Charybdotoxin / toxicity
  • Cricetinae
  • Cricetulus
  • Humans
  • Kv1.3 Potassium Channel / antagonists & inhibitors*
  • Kv1.3 Potassium Channel / chemistry
  • Large-Conductance Calcium-Activated Potassium Channels / antagonists & inhibitors*
  • Large-Conductance Calcium-Activated Potassium Channels / chemistry
  • Molecular Sequence Data
  • Peptides / chemistry
  • Peptides / toxicity
  • Potassium Channel Blockers / chemistry*
  • Potassium Channel Blockers / toxicity*
  • Scorpion Venoms / chemistry*
  • Scorpion Venoms / genetics
  • Scorpion Venoms / toxicity*

Substances

  • Kv1.3 Potassium Channel
  • Large-Conductance Calcium-Activated Potassium Channels
  • Peptides
  • Potassium Channel Blockers
  • Scorpion Venoms
  • hongotoxin 1
  • Charybdotoxin
  • iberiotoxin