Towards the discovery of novel T-type calcium channel blockers

Authors: Lory, Philippe; Chemin, Jean

Source: Expert Opinion on Therapeutic Targets, Volume 11, Number 5, May 2007 , pp. 717-722(6)

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Abstract:

Despite their presence in many tissues and their potential implication in various disease states, low-voltage activated T-type calcium channels (T-channels) have only recently become targets of interest. Unfortunately, the lack of selective T-channel blockers has hampered further characterisation of these channels. The recent availability of cloned T-channels, the Ca_V3 proteins, facilitates identification of novel T-channel blockers. Also, studies performed in knockout animals have fostered novel interest. Selective inhibition of T-channels may have clinical importance in cardiovascular diseases, some forms of epilepsy, sleep disorders, pain and possibly cancer. This review focuses on novel research approaches to discover potent and selective T-channel modulators. These molecules may be potential drugs for treating human diseases, as well as important tools to decipher the physiological role of these channels.

Keywords: CaV3 subunit; low-voltage activated; T-type calcium channel

Document Type: Research article

DOI: http://dx.doi.org/10.1517/14728222.11.5.717

Affiliations: 1: Institut de Génomique Fonctionnelle (IGF), Département de Physiologie, CNRS UMR 5203 - INSERM U661 - IFR3 - Universités de Montpellier I and II, 141 rue de la Cardonille, 34094 Montpellier cedex 05, France., Email: philippe.lory@igf.cnrs.fr

Publication date: 2007-05-01

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