Exploiting the Diversity of Ion Channels: Modulation of Ion Channels for Therapeutic Indications

Handb Exp Pharmacol. 2019:260:187-205. doi: 10.1007/164_2019_333.

Abstract

Ion channels are macromolecular proteins that form water-filled pores in cell membranes and they are critical for a variety of physiological and pharmacological functions. Dysfunctional ion channels can cause diseases known as channelopathies. Ion channels are encoded by approximately 400 genes, representing the second largest class of proven drug targets for therapeutic areas including neuropsychiatric disorders, cardiovascular and metabolic diseases, immunological diseases, nephrological diseases, gastrointestinal diseases, pulmonary/respiratory diseases, and many cancers. With more ion channel structures are being solved and functional robust assays are being developed, there are tremendous opportunities for identifying specific modulators targeting ion channels for new therapy.

Keywords: ANO1; Arrhythmia; BK; CFTR; Cancer; Channelopathy; Drug target; Epilepsy; GABA; KCNQ; Kir; Kv7; LRRC8A; Nav; Pain; TMEM16A; hERG.

Publication types

  • Review

MeSH terms

  • Channelopathies / drug therapy*
  • Humans
  • Ion Channels / agonists*
  • Ion Channels / antagonists & inhibitors*
  • Molecular Targeted Therapy*

Substances

  • Ion Channels