Generic placeholder image

Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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

Author(s): Hiroyuki Miyachi

Volume 14 , Issue 22 , 2007

Page: [2335 - 2343] Pages: 9

DOI: 10.2174/092986707781745587

Price: $65

Abstract

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


Rights & Permissions Print Export Cite as
© 2022 Bentham Science Publishers | Privacy Policy