Pregnane X receptor (PXR)-multidrug resistance-associated protection (MRP2) luciferase reporter gene-expressing technical platform high-flux medicament screening method

2010 
The invention discloses a pregnane X receptor (PXR)-multidrug resistance-associated protection (MRP2) luciferase reporter gene-expressing technical platform high-flux medicament screening method, which screens candidate potential activity pilot medicaments by directly starting from a medicament metabolism dynamic target which is used in a terminal medicament clinic research stage in a new medicament research. In the method, a luciferase reporter gene containing a MRP2 gene promoter sequence and expression plasmids of RXR is constructed and human hepatocellular carcinoma (HepG 2) cells are transfected transiently; and the high-flux screening of in-vitro RXR induction potential activity pilot medicaments is carried out by detecting the activity of the luciferase in a self-luminous detector and reflecting the influences of different potential activity pilot medicaments on the activity of a MRP2 promoter according to the ratio of the fluorescence of a glowworm to the fluorescence of a sea pansy. The method can avoid severe untoward effects aroused by activity medicaments obtained by other medicament screening methods due to medicament interaction generated in a final clinical medication process, save a big amount of preliminary investment in the new medicament research and reduce blindness.
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