Effects of structural and electronic characteristics of chalcones on the activation of peroxisome proliferator-activated receptor gamma (PPARγ)

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概要

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• Chalcones share some structural similarities with GW-1929, a highly-selective and a potent agonist for peroxisome proliferator-activated receptor-gamma (PPARγ). In this study, we tested 53 structurally diverse chalcones to identify characteristics essential for PPARγ activation in a GAL4-based transactivation assay. This screen identified several novel chalcone agonists of PPARγ.Our results indicate that chalcones with an electron rich group or sterically large groups such as napthyl on the carbonyl side tend to activate PPARγ.The absence of any strict structural or electronic requirements suggests that the flexibility of the PPARγ ligand binding pocket may allow binding of diverse chalcones with some preference for a slightly larger electron-rich group on the carbonyl side. We predict that further structure-activity-relationship (SAR) studies on chalcones with naphthalene or electron-rich groups near the carbonyl moiety will lead to the development of more potent PPARγ agonists.

著者

• Chen Kevin

  Department Of Electrical And Electronic Engineering Hong Kong University Of Science And Technology

• Leon Martin

  Department of Chemistry, California State University

• Schott Jason

  Department of Biological Science, California State University

• Mordaunt Charles

  Department of Biological Science, California State University

• Vargas Anthony

  Department of Biological Science, California State University

• Singh Mandeep

  Department of Chemistry, California State University

• Satoh Mikiko

  Department of Chemistry and Biochemistry, California State University

• Cardenas Emilio

  Department of Chemistry, California State University

• Maitra Santanu

  Department of Chemistry, California State University

• Patel Nilay

  Center for Applied Biotechnology Studies, California State University

• de Lijser

  Department of Chemistry and Biochemistry, California State University

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