Methods for identifying modulators of n-type ion channel...

Details Methods for identifying modulators of n-type ion channel... Methods for identifying modulators of n-type ion channel...

C - Chemistry, Metallurgy

12

N

C12N 15/12 (2006.01) C07H 21/04 (2006.01) C12N 1/00 (2006.01) C12N 1/14 (2006.01) C12N 15/63 (2006.01) C12Q 1/02 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2370615

Methods and compositions for identifying compounds which disrupt the functional interaction of an intracellular receptor region of an .alpha.- subunit of a voltage-gated ion channel and an amino-terminal inactivation region of an ion channel protein are disclosed. Compounds that disrupt the functional or binding interaction of these two regions have significant modulatory effects on ion channel activity, and thus are likely to be useful for treating and/or preventing a wide variety of diseases and pathological conditions associated with ion channel dysfunction. Such conditions include, for example, neurological disorders, cardiac diseases, metabolic diseases, tumor-driven diseases, and autoimmune diseases.

L'invention concerne des procédés et des compositions destinées à identifier des composés qui désorganisent l'interaction fonctionnelle d'une région intracellulaire réceptrice d'une sous-unité alpha d'un canal ionique potentiel-dépendant et d'une région d'inactivation amino-terminale d'une protéine à canal ionique. Les composés désorganisant l'interaction fonctionnelle ou l'interaction de fixation de ces deux régions exercent une puissante action modulatrice sur l'activité des canaux ioniques, et peuvent donc être utiles dans le traitement et/ou la prévention d'une grande diversité de maladies et d'états pathologiques liés à un dysfonctionnement des canaux ioniques. Parmi ces états pathologiques, figurent notamment les troubles neurologiques, les maladies du coeur, les maladies métaboliques, les maladies induites par une tumeur et les maladies auto-immunes.

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