Prospects for rational development of pharmacological gap junction channel blockers

Curr Drug Targets. 2002 Dec;3(6):455-64. doi: 10.2174/1389450023347353.


Connexin-null mice and human genetic gap junction diseases illustrate the important roles that gap junction channels play under normal conditions, and the neuro- and cardioprotective effects of gap junction blocking agents demonstrate that closure of these channels may be beneficial in certain pathological situations. This overview summarizes studies in which gap junction modifying reagents have been characterized, highlighting examples of agents for which selectivity for gap junction subtypes has been demonstrated. In addition, strategies for targeting connexin domains through peptide inhibitors are outlined, which may ultimately provide agents that are not only connexin-selective in their actions, but also affect only a subset of a gap junction channel's gating responses.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Connexins / antagonists & inhibitors*
  • Connexins / metabolism
  • Drug Delivery Systems / methods*
  • Gap Junctions / metabolism
  • Humans
  • Ion Channels / antagonists & inhibitors*
  • Ion Channels / metabolism


  • Connexins
  • Ion Channels