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Current Drug Targets


ISSN (Print): 1389-4501
ISSN (Online): 1873-5592

Prospects for Rational Development of Pharmacological Gap Junction Channel Blockers

Author(s): David C. Spray, Renato Rozental and Miduturu Srinivas

Volume 3, Issue 6, 2002

Page: [455 - 464] Pages: 10

DOI: 10.2174/1389450023347353

Price: $65


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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