Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Notes
Structure-Based Design and Synthesis of Fluorescent PPARα/δ Co-agonist and Its Application as a Probe for Fluorescent Polarization Assay of PPARδ Ligands
Yoko Araya, Jun-ichi Kasuga, Kenji Toyota, Yuko Hirakawa, Takuji Oyama, Makoto Makishima, Kosuke Morikawa, Yuichi Hashimoto, Hiroyuki Miyachi
著者情報
キーワード: fluorescent ligand, phenylpropanoic acid, fluorescent polarization, peroxisome proliferator-activated receptor, fluorescent peroxisome proliferator-activated receptor α/δ co-agonist
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2008 年 56 巻 9 号 p. 1357-1359

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Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARα/δ) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARα/δ co-agonist, which has a pyrene unit incorporated directly at the hydrophobic tail part of the structure as a fluorophore. This fluorescent co-agonist was applied in a homogeneous fluorescent polarization assay format for the identification of PPARδ ligands.
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© 2008 The Pharmaceutical Society of Japan
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