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Adaptability and selectivity of human peroxisome proliferator-activated receptor (PPAR) pan agonists revealed from crystal structures
The structures of the ligand-binding domains (LBDs) of human peroxisome proliferator-activated receptors (PPARα, PPARγ and PPARδ) in complexes with a pan agonist, an α/δ dual agonist and a
Structure-Based Design and Synthesis of Fluorescent PPARα/δ Co-agonist and Its Application as a Probe for Fluorescent Polarization Assay of PPARδ Ligands
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
Structure-based design and synthesis of fluorescent PPARalpha/delta co-agonist and its application as a probe for fluorescent polarization assay of PPARdelta ligands.
TLDR
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, was designed and synthesized.