Synthetic ligands for peroxisome proliferator-activated receptor-α, review of the patent literature 2000 - 2003

Hiroyuki Miyachi

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

The identification of the nuclear receptor peroxisome proliferator-activated receptor-alpha (PPARα) as a molecular target of the fibrate class of anti-dyslipidaemic agents and the rapid development of the parallel high-through-put approach to evaluate activity towards other PPAR subtypes (PPARδ and PPARΥ) has provided an opportunity to develop novel PPARα-selective, PPARα/Υ dual and pan-PPAR agonists. This review outlines the molecular pharmacology of PPARα and summarises recent patents (from 2000 to 2003) disclosing medicinal chemical strategies to identify new PPARα agonists. These developments will help us to understand the structure-activity relationship and the interaction between the ligands and PPARα and also help to create novel therapeutic choices for the treatment of metabolic disorders, such as dyslipidaemia, obesity, diabetes and other PPARα-related diseases. 2004

Original languageEnglish
Pages (from-to)607-618
Number of pages12
JournalExpert Opinion on Therapeutic Patents
Volume14
Issue number5
DOIs
Publication statusPublished - May 2004
Externally publishedYes

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Keywords

  • α-substituted phenylpropanoic acid
  • Carboxylic acid
  • Dyslipidaemia
  • Peroxisome proliferator-activated receptor-α (PPARα)
  • Phenoxyacetic acid
  • Thiazolidine-2,4-dione

ASJC Scopus subject areas

  • Medicine (miscellaneous)
  • Pharmacology
  • Law

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