Voltage-gated potassium channels as therapeutic targets

Nat Rev Drug Discov. 2009 Dec;8(12):982-1001. doi: 10.1038/nrd2983.


The human genome encodes 40 voltage-gated K(+) channels (K(V)), which are involved in diverse physiological processes ranging from repolarization of neuronal and cardiac action potentials, to regulating Ca(2+) signalling and cell volume, to driving cellular proliferation and migration. K(V) channels offer tremendous opportunities for the development of new drugs to treat cancer, autoimmune diseases and metabolic, neurological and cardiovascular disorders. This Review discusses pharmacological strategies for targeting K(V) channels with venom peptides, antibodies and small molecules, and highlights recent progress in the preclinical and clinical development of drugs targeting the K(V)1 subfamily, the K(V)7 subfamily (also known as KCNQ), K(V)10.1 (also known as EAG1 and KCNH1) and K(V)11.1 (also known as HERG and KCNH2) channels.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antibodies / pharmacology
  • Clinical Trials as Topic
  • Drug Delivery Systems*
  • Drug Design*
  • Drug Evaluation, Preclinical
  • Humans
  • Peptides / pharmacology
  • Potassium Channels, Voltage-Gated / drug effects*
  • Potassium Channels, Voltage-Gated / metabolism
  • Signal Transduction / drug effects
  • Venoms / pharmacology


  • Antibodies
  • Peptides
  • Potassium Channels, Voltage-Gated
  • Venoms