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Design, Synthesis, and Structure-Activity Relationship Study of Peroxisome Proliferator-Activated Receptor (PPAR) δ-Selective Ligands

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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.

Keywords: GW-501516; PPAR; PPARδ; PPARδ selective agonist; Peroxisome proliferator-activated receptor; TIPP-204; metabolic syndrome

Document Type: Research Article


Affiliations: Institute of Molecular and Cellular Biosciences, University of Tokyo, Yayoi Bunkyo-ku, Tokyo, 113-0032, Japan.

Publication date: 2007-09-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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