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Review
. 2017 Dec;180:144-160.
doi: 10.1016/j.pharmthera.2017.07.001. Epub 2017 Jul 15.

Inhibitors of Connexin and Pannexin Channels as Potential Therapeutics

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Free PMC article
Review

Inhibitors of Connexin and Pannexin Channels as Potential Therapeutics

Joost Willebrords et al. Pharmacol Ther. .
Free PMC article

Abstract

While gap junctions support the exchange of a number of molecules between neighboring cells, connexin hemichannels provide communication between the cytosol and the extracellular environment of an individual cell. The latter equally holds true for channels composed of pannexin proteins, which display an architecture reminiscent of connexin hemichannels. In physiological conditions, gap junctions are usually open, while connexin hemichannels and, to a lesser extent, pannexin channels are typically closed, yet they can be activated by a number of pathological triggers. Several agents are available to inhibit channels built up by connexin and pannexin proteins, including alcoholic substances, glycyrrhetinic acid, anesthetics and fatty acids. These compounds not always strictly distinguish between gap junctions, connexin hemichannels and pannexin channels, and may have effects on other targets as well. An exception lies with mimetic peptides, which reproduce specific amino acid sequences in connexin or pannexin primary protein structure. In this paper, a state-of-the-art overview is provided on inhibitors of cellular channels consisting of connexins and pannexins with specific focus on their mode-of-action and therapeutic potential.

Keywords: Connexin; Gap junction; Hemichannel; Inhibitor; Pannexin.

Conflict of interest statement

Conflict of Interest statement

The authors declare that there are no conflicts of interest.

Figures

Figure 1
Figure 1
Connexin and pannexin structure.
Figure 2
Figure 2
Mimetic peptides targeting connexin and pannexin channels.

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