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The luciferase cellular assay was used as a primary screen. We also measured ApoA1 secretion as a secondary assay in the same cell type. A very nice correlation between the two readouts was observed, indicating that compounds were truly upregulators of ApoA1 production by hepatic cells. See Supplementary data for details
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The luciferase cellular assay was used as a primary screen. We also measured ApoA1 secretion as a secondary assay in the same cell type. A very nice correlation between the two readouts was observed, indicating that compounds were truly upregulators of ApoA1 production by hepatic cells. See Supplementary data for details.
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A combination of our ApoA1 upregulators with statins has been envisaged. Since Cytochrome P450 (CYP) isoenzymes are involved in the oxidative metabolism of the statins, with CYP3A4 and CYP2C9 isoenzymes being the most dominant, we wanted to discharge any risk of drug-drug interactions with our compounds being CYP inhibitors. See Bellosta, S.; Paoletti, R.; and Corsini A. Circulation 2004, 109, III-50
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