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Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARalpha/delta) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARalpha/delta co-agonist, which has a pyrene unit incorporated directly at the hydrophobic tail part of the structure as a fluorophore. This fluorescent co-agonist was applied in a homogeneous fluorescent polarization assay format for the identification of PPARdelta ligands.

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Structure-Based Design and Synthesis of Fluorescent PPAR.ALPHA./.DELTA. Co-agonist and Its Application as a Probe for Fluorescent Polarization Assay of PPAR.DELTA. Ligands