Recent progress of the research on peroxisome proliferator-activated receptor α-selective ligands

Hiroyuki Miyachi

Research output: Contribution to journalArticle

3 Citations (Scopus)


The understanding of the functions of the nuclear receptor peroxisome proliferator-activated receptor a (PPARalpha) as a regulator of lipid and lipoprotein homeostasis, and the rapid development of parallel high-throughput screening assays to evaluate the activity toward other PPAR subtypes (PPARdelta and PPARgamma), have provided an opportunity to develop novel PPARalpha-selective, PPARalpha/gamma dual and PPAR pan agonists for the treatment of various metabolic diseases. This review focuses on the molecular pharmacology of PPARalpha, and summarizes recent literature and patent applications disclosing medicinal chemistry strategies to identify new PPARalpha-selective agonists. The species selectivity of some classes of PPARalpha-selective agonists in response to in vitro PPARalpha transactivation activity is also reported.

Original languageEnglish
Pages (from-to)746-754
Number of pages9
Issue number8
Publication statusPublished - Aug 1 2004



  • Metabolic disorders
  • Peroxisome proliferatoractivated receptorα
  • Phenoxyacetic acid
  • Species selectivity

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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