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Abstract The farnesoid X receptor (FXR) is a nuclear receptor that controls bile acid, lipid, and cholesterol metabolism. FXR-targeted drugs have shown promise in late-stage clinical trials for non-alcoholic steatohepatitis.
Materials and Methods A biochemical ligand-dependent nuclear receptor-cofactor peptide interaction assay was conducted as described (Hambruch et al., 2012), with biotinylated SRC-1 peptide b-CPSSHSSLTERHKILHRLLQEGSPS-COOH (0.4 µM) and purified FXRaa187–472-LBD fused to glutathione S-transferase (2.5 ng) together with 200 ng streptavidine-allophycocyanin and 6 ng europium labeled-anti-glutathione S-transferase as reagents in 25 µl assay buffer (20 mM Tris/HCl at pH 7.5; 5 mM MgCl2; 60 mM KCl;...
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