Fluorescence based assay to detect sodium/calcium exchanger ''forward mode'' modulating compounds
A technology of exchangers and compounds, which is applied in the field of sodium/calcium exchangers and detection of their activity, can solve the problems of limited turnover of ion transporters and other problems
Inactive Publication Date: 2011-02-16
SANOFI AVENTIS SA
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Problems solved by technology
[0014] The main problem with radiometric assays arises from the difficulty in detecting the limited turnover (about 104 times less than most ion channels) of ion transporters at about 1-1000 molecules per second
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[0083] 1. Measurement steps
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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 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.
Description
field of invention [0001] The present invention relates to sodium / calcium exchangers and methods for detecting their activity. More specifically, the present invention relates to fluorescence-based assays for the detection of "forward mode" modulating compounds of sodium / calcium exchangers. The invention also relates to a kit of parts comprising cells expressing a sodium / calcium exchanger and to the use of the kit of parts. Background of the invention [0002] A fundamental necessity of life is compartmentalization - with biofilms as a natural tool to achieve this principle. However, the lipid bilayer—the structure that forms the basis of cell membranes—is impermeable to most ions and compounds whose transport is necessary to maintain the vital functions of cells and organisms. The answer to this paradox lies in the semipermeable nature of cell membranes—solutes that must cross the membrane are transported by specific membrane proteins. These transporters are responsible ...
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IPC IPC(8): G01N33/68
CPCG01N2500/10G01N33/6872
Inventor M·胡格T·利歇尔S·盖贝尔H·福勒特
Owner SANOFI AVENTIS SA