Prospects for rational development of pharmacological gap junction channel blockers

David C. Spray, Renato Rozental, Miduturu Srinivas

Research output: Contribution to journalReview article

68 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)455-464
Number of pages10
JournalCurrent drug targets
Volume3
Issue number6
DOIs
StatePublished - Dec 1 2002

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

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