Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARα/δ) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARα/δ 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 PPARδ ligands.
- Fluorescent ligand
- Fluorescent peroxisome proliferator-activated receptor α/δ co-agonist
- Fluorescent polarization
- Peroxisome proliferator-activated receptor
- Phenylpropanoic acid
ASJC Scopus subject areas
- Drug Discovery