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 channels gating responses.
Current Drug Targets
Title: Prospects for Rational Development of Pharmacological Gap Junction Channel Blockers
Volume: 3 Issue: 6
Author(s): David C. Spray, Renato Rozental and Miduturu Srinivas
Affiliation:
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 channels gating responses.
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Cite this article as:
David C. Spray , Renato Rozental and Miduturu Srinivas , Prospects for Rational Development of Pharmacological Gap Junction Channel Blockers, Current Drug Targets 2002; 3 (6) . https://dx.doi.org/10.2174/1389450023347353
DOI https://dx.doi.org/10.2174/1389450023347353 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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