Abstract
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.
Original language | English |
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Pages (from-to) | 1357-1359 |
Number of pages | 3 |
Journal | Chemical and Pharmaceutical Bulletin |
Volume | 56 |
Issue number | 9 |
DOIs | |
Publication status | Published - Sep 2008 |
Keywords
- Fluorescent ligand
- Fluorescent peroxisome proliferator-activated receptor α/δ co-agonist
- Fluorescent polarization
- Peroxisome proliferator-activated receptor
- Phenylpropanoic acid
ASJC Scopus subject areas
- Chemistry(all)
- Drug Discovery