The voltage-gated potassium channel Kv1.3 is a promising multitherapeutic target against human pathologies

Expert Opin Ther Targets. 2016;20(5):577-91. doi: 10.1517/14728222.2016.1112792. Epub 2015 Dec 4.

Abstract

Introduction: The voltage-dependent potassium channel Kv1.3 is mainly present in the nervous and immune systems. In leukocytes, Kv1.3 fine-tunes the activation and proliferation of the immune response. However, Kv1.3 is also present in other tissues where its physiological role is still under investigation. Thus, Kv1.3 alterations have been related to several human diseases.

Areas covered: In this work, the authors highlight the role of Kv1.3 in various pathologies and the potential use of Kv1.3 blockers as safe pharmacological tools. The limited repertoire of K(+) channels in leukocytes and its expression pattern makes Kv1.3 crucial for effector memory T cell physiology and it is therefore a good pharmacological target for chronic inflammatory diseases. Moreover, Kv1.3 has been related to insulin sensitivity, cell proliferation and apoptosis. In this scenario, Kv1.3 activity is also implicated in non-insulin-dependent type II diabetes mellitus, obesity and cancer.

Expert opinion: Fortunately, Kv1.3 is characterized by a very selective and potent pharmacology that has been demonstrated to ameliorate autoimmune and metabolic symptoms in disease-animal models without major side effects. Moreover, Kv1.3 blockers are showing positive results in preclinical trials. Considering this evidence, the implication of Kv1.3 in a wide repertoire of human pathologies indicates this channel is an important therapeutic target.

Keywords: Autoimmune diseases; Kv1.3 blockers; cancer; clinical trials; inflammatory disorders; obesity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Autoimmune Diseases / drug therapy
  • Autoimmune Diseases / metabolism
  • Humans
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Kv1.3 Potassium Channel / antagonists & inhibitors
  • Kv1.3 Potassium Channel / metabolism*
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Obesity / drug therapy
  • Obesity / metabolism
  • Potassium Channel Blockers / therapeutic use

Substances

  • Kv1.3 Potassium Channel
  • Potassium Channel Blockers