Patent ID: 8609329

Claim:
A method for screening compounds that inhibit intracellular release of low density lipoprotein-cholesterol (LDL-C) from a LDL receptor (LDL-R), the method comprising the steps: a) providing a monolayer of cells that have LDL-R in the plasma membrane (PM) of said cells; b) in the presence of a compound to be tested, incubating said cells with a first population of LDL-C that is labeled with a donor fluorophore (D) and a second population of LDL-C that is labeled with an acceptor (A) fluorophore, for a time sufficient for binding of LDL-C to LDL-R to form a LDL-R/LDL-C complex on the surface of said cells; c) incubating said cells for a time sufficient for internalization of the LDL-R/LDL-C complex into said cells; d) using FRET-confocal microscopy imaging, determining intensity values for D and A and the efficiency of energy transfer (E %) to determine whether LDL-R/LDL-C complexes in the endosomal membrane have a random distribution or a clustered distribution, wherein a random distribution indicates release of LDL-C from LDL-R and a clustered distribution indicates that the compound tested inhibits LDL-C release from the LDL-R/LDL-C complex.