Structure-based design and synthesis of fluorescent PPARα/δ co-agonist and its application as a probe for fluorescent polarization assay of PPARδ ligands

Yoko Araya, Jun Ichi Kasuga, Kenji Toyota, Yuko Hirakawa, Takuji Oyama, Makoto Makishima, Kosuke Morikawa, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

11 Citations (Scopus)

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 languageEnglish
Pages (from-to)1357-1359
Number of pages3
JournalChemical and Pharmaceutical Bulletin
Volume56
Issue number9
DOIs
Publication statusPublished - Sep 2008
Externally publishedYes

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Keywords

  • 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
  • Organic Chemistry
  • Chemistry(all)
  • Pharmacology

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