Fluorescence based assay to detect sodium/calcium exchanger...

Details Fluorescence based assay to detect sodium/calcium exchanger... Fluorescence based assay to detect sodium/calcium exchanger...

G - Physics

01

N

G01N 33/58 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2718734

Transporters are an emerging target family with enormous potential, offering scientific and economic opportunities. The sodium/calcium exchanger is an important mechanism for removing Ca2+" from diverse cells. In heart, it extrudes Ca2+ that has entered through Ca2+ channels to initiate contraction, while Na+ enters the heart cell. It is of considerable interest to identify compounds that modulate, not only the calcium export activity (forward mode), but also the calcium import activity (reverse mode) of sodium/calcium exchangers. The present invention is directed to a fluorescence-based assay for detecting NCX "reverse mode" modulating compounds. It further refers to a kit of parts comprising cells expriming NCX and the use of the kit of parts to test a compound for activity as an agonist or antagonist of NCX.

L'invention porte sur des transporteurs qui sont une famille cible émergente avec un énorme potentiel, offrant des opportunités scientifiques et économiques. L'échangeur de sodium/calcium est un mécanisme important pour éliminer le Ca2+ de diverses cellules. Dans le cur, il extrude le Ca2+ qui est entré par les canaux de Ca2+ pour initier une contraction, tandis que le Na+ entre dans la cellule cardiaque. Il est d'un intérêt considérable d'identifier des composés qui modulent non seulement l'activité d'export de calcium (mode direct), mais encore l'activité d'import de calcium (mode inverse) des échangeurs de sodium/calcium. La présente invention porte sur un essai à base de fluorescence pour détecter des composés modulant le « mode inverse » de NCX. Elle porte en outre sur un coffret de parties comprenant des cellules exprimant NCX et sur l'utilisation du coffret de parties pour tester un composé pour l'activité en tant qu'agoniste ou antagoniste de NCX.

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