FLUORESCENCE BASED ASSAY TO DETECT SODIUM/CALCIUM EXCHANGER FORWARD MODE MODULATING COMPOUNDS

摘要

Transporters are an emerging target family with enormous potential, offering scientific and economic opportunities. The sodium/calcium exchanger is an important mechanism for removing Ca 2+ from diverse cells. In heart, it extrudes Ca 2+ that has entered through Ca 2+ channels to initiate contraction, while Na + enters the heart cell. It is of considerable interest to identify compounds that modulate the activity of sodium/calcium exchangers. The present invention is directed to a fluorescence-based assay for detecting NCX and NCKX "forward mode" modulating compounds. It further refers to a kit of parts comprising cells expriming a sodium/calcium exchanger and the use of the kit of parts to test a compound for activity as an agonist or antagonist of a sodium/calcium exchanger.