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Keywords:

  • channelopathy;
  • ion channels;
  • hERG;
  • high-throughput electrophysiology;
  • NaV1.7;
  • P2X4;
  • pain;
  • TREK1;
  • TRESK;
  • TRPV1

Abstract

Objectives  This review considers ion channels as potential novel therapeutic targets, particularly in the treatment of pain.

Key findings  Ion channel proteins underlie electrical signalling throughout the body and are important targets for existing therapeutic agents. Nevertheless, ion channels remain a relatively underexploited family of proteins for therapeutic interventions. A number of recent advances in both technology and knowledge suggest that these proteins are promising targets for future therapeutic development. For example, there has been considerable recent improvement in high-throughput screening technologies following the need for pharmaceutical companies to screen against compounds which block human ether-a-go-go-related gene (hERG) potassium channels. Similarly an increased awareness of the importance of ion channels in disease states such as epilepsy, ataxia, cardiac arrhythmia, diabetes and cystic fibrosis has been revealed through studies of genetic mutations in humans and genetic ablation studies in animals. Furthermore, recent advances in the understanding of ion channel structure and how this relates to their function has provided significant new insights into where exactly on the ion channel protein novel therapeutic agents might be developed to target. In the particular area of pain research a number of different ion channel subtypes have been identified (including certain sodium, potassium and transient receptor potential (TRP) channels).

Summary  It seems likely that new therapies will arise that target ion channels. In the treatment of pain, for example, novel agents targeting TRPV1 channels are already showing considerable therapeutic promise.