Crac modulators and use of same for drug discovery

Details Crac modulators and use of same for drug discovery Crac modulators and use of same for drug discovery

C - Chemistry, Metallurgy

12

Q

C12Q 1/02 (2006.01) C12Q 1/68 (2006.01) G01N 33/567 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2648588

The invention relates to use of a calcium release activated Ca+2 (CRAC) channel (CRACM) such as CRACM1 and CRACM2 to identify bioactive agents which can modulate store operated calcium entry and CRAC channel activity. The invention further relates to the use of recombinant nucleic acids that encode CRACM. One aspect of the invention includes methods of determining binding of candidate bioactive agents to a CRACM polypeptide and for determining modulation of CRACM polypeptide activity as it affects CRAC channel permeability. The invention further relates to methods and compositions modulating the cellular expression of the nucleic acids that encode CRACM.

L'invention concerne l'utilisation de modulateurs (CRACM) de canal Ca2+ activé par libération de calcium (CRAC), tels que les modulateurs CRACM1 et CRACM2, pour identifier des agents bioactifs pouvant moduler l'influx calcique induit par réserve et l'activité du canal CRAC. L'invention concerne en outre l'utilisation d'acides nucléiques recombinants qui codent pour CRACM. Un aspect de l'invention concerne des procédés pour déterminer la liaison d'agents bioactifs candidats avec un polypeptide CRACM et pour déterminer la modulation de l'activité d'un polypeptide CRACM, affectant la perméabilité du canal CRAC. L'invention concerne par ailleurs des procédés et des compositions modulant l'expression cellulaire des acides nucléiques codant pour CRACM.

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