Design, synthesis, and structure-activity relationship study of peroxisome proliferator-activated receptor (PPAR) δ-selective ligands

Hiroyuki Miyachi

研究成果査読

13 被引用数 (Scopus)

抄録

Improvements in our understanding of the functions of peroxisome proliferator-activated receptor (PPAR) subtypes as master regulators of many biological functions have made it possible to develop novel PPAR ligands with characteristic subtype selectivity as biochemical tools and/ or candidatedrugs for the treatment of PPAR-dependent diseases such as metabolic syndrome, which includes type II diabetes, dyslipidemia, obesity, hypertension, and inflammation. Based on the findings that the glitazone-class antidiabetic agents, and fibrate-class antidyslipidemic agents are ligands of PPARγ and PPARα: respectively, much research interest has been focused on these two subtypes as therapeutic targets for the treatment of type II diabetes and dyslipidemia. In contrast, research interest in PPARδ has, been limited. However, since 2001, the availability of PPARδ knockout animals and selective ligands has led to the uncovering of possible roles of PPARδ in fatty acid metabolism, insulin resistance, reverse cholesterol transport, inflammation, and so on. It has become clear that ligands able to modulate PPARδ-mediated pathways are candidates for the treatment of altered metabolic function. This review focuses on recent medicinal chemical studies to identify PPARδ-selective agonists.

本文言語English
ページ(範囲)2335-2343
ページ数9
ジャーナルCurrent Medicinal Chemistry
14
22
DOI
出版ステータスPublished - 9月 2007
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 薬理学
  • 創薬
  • 有機化学

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