Methods of screening for ltrpc7 modulators

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 15/12 (2006.01) C07K 14/705 (2006.01) G01N 33/53 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2428698

The present invention relates to the identification and isolation of a novel family of ATP regulated calcium transmembrane channel polypeptides designated herein as "LTRPC7" (Long Transient Receptor Potential Channel). Channels comprising these polypeptides close in response to concentrations of cytoplasmic ATP in the millimolar range, are subject to inhibition by high intracellular levels of calcium and/or magnesium, and do not respond to depletion or reduction in intracellular calcium stores. The invention further relates to the methods of utilizing LTRPC7 for binding, and the methods for modulating LTRPC7 activity and for measuring LTRPC2 permeability. The invention further relates to the methods of modulating expression of LTRPC7.

La présente invention se rapporte à l'identification et l'isolation d'une nouvelle famille de polypeptides canal transmembranaires régulés par ATP, désignés dans l'invention par "LTRPC7" (canal de potentiel de récepteur transitoire long). Les canaux comprenant ces polypeptides se ferment en présence de concentrations d'ATP cytoplasmique dans la gamme millimolaire, sont sujet à l'inhibition par des taux intracellulaires élevés de calcium et/ou de magnésium et ne réagissent pas à la déplétion ou la réduction dans des stocks de calcium intracellulaires. L'invention concerne en outre des procédés pour utiliser LTRPC7 pour lier ou moduler d'autres manières l'activité de LTRPC7 et mesurer la perméabilité de LTRPC2. Elle concerne en outre des procédés pour moduler l'expression de LTRPC7.

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