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Review
. 2010 Jul;11(7):761-70.

The alpha2-delta protein: an auxiliary subunit of voltage-dependent calcium channels as a recognized drug target

Affiliations
  • PMID: 20571971
Review

The alpha2-delta protein: an auxiliary subunit of voltage-dependent calcium channels as a recognized drug target

Andrew J Thorpe et al. Curr Opin Investig Drugs. 2010 Jul.

Abstract

Currently, there are two drugs on the market, gabapentin (Neurontin) and pregabalin (Lyrica), that are proposed to exert their therapeutic effect through binding to the alpha2-delta subunit of voltage-sensitive calcium channels. This activity was unexpected, as the alpha2-delta subunit had previously been considered not to be a pharmacological target. In this review, the role of the alpha2-delta subunits is discussed and the mechanism of action of the alpha2-delta ligands in vitro and in vivo is summarized. Finally, new insights into the mechanism of drugs that bind to this protein are discussed.

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