Fluorescence-based assay for detecting compounds for...

Details Fluorescence-based assay for detecting compounds for... Fluorescence-based assay for detecting compounds for...

G - Physics

01

N

G01N 33/68 (2006.01)

Patent

CA 2680768

Carriers are an up-and-coming target family with enormous potential and offer commercial and scientific possibilities. The sodium/calcium exchanger is an important mechanism for the removal of Ca2+ from various cells. In the heart, said sodium/calcium exchanger extrudes Ca2+, which has entered through Ca2+ channels for the initiation of contractions, while Na+ enters the heart cell. It is of considerable interest to identify compounds that modulate the activity of the sodium-calcium exchanger. The present invention relates to a fluorescence-based assay for the detection of compounds for modulating the NCX in ~forward mode.~ The invention further relates to a parts set comprising cells that express NCX and to the use of said parts set for testing a compound for activity as an agonist or antagonist of NCX.

Les transporteurs constituent une famille cible en pleine croissance ayant un potentiel énorme, offrant des possibilités scientifiques et économiques. L'échangeur de sodium/calcium est un mécanisme important pour l'extraction de Ca2+ à partir de diverses cellules. Dans le coeur, cet échangeur extrude Ca2+ ayant pénétré par des canaux de Ca2+ pour le déclenchement d'une contraction, tandis que Na+ pénètre dans la cellule cardiaque. Il est très intéressant d'identifier des composés modulant l'activité de l'échangeur de sodium-calcium. L'invention concerne un dosage biologique à base de fluorescence pour l'identification de composés modulant l'échangeur de sodium-calcium (NCX) dans le "mode d'avancement". L'invention concerne par ailleurs un ensemble comportant des cellules exprimant NCX et l'utilisation de l'ensemble pour le test d'un composé en ce qui concerne son activité en tant qu'agoniste ou antagoniste de NCX.

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