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

doi:10.1248/cpb.56.1357

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

Faculty of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

14 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	1357-1359
Number of pages	3
Journal	Chemical and Pharmaceutical Bulletin
Volume	56
Issue number	9
DOIs	https://doi.org/10.1248/cpb.56.1357
Publication status	Published - Sep 2008

Keywords

Fluorescent ligand
Fluorescent peroxisome proliferator-activated receptor α/δ co-agonist
Fluorescent polarization
Peroxisome proliferator-activated receptor
Phenylpropanoic acid

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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Araya, Y., Kasuga, J. I., Toyota, K., Hirakawa, Y., Oyama, T., Makishima, M., Morikawa, K., Hashimoto, Y., & Miyachi, H. (2008). Structure-based design and synthesis of fluorescent PPARα/δ co-agonist and its application as a probe for fluorescent polarization assay of PPARδ ligands. Chemical and Pharmaceutical Bulletin, 56(9), 1357-1359. https://doi.org/10.1248/cpb.56.1357

Araya, Y, Kasuga, JI, Toyota, K, Hirakawa, Y, Oyama, T, Makishima, M, Morikawa, K, Hashimoto, Y & Miyachi, H 2008, 'Structure-based design and synthesis of fluorescent PPARα/δ co-agonist and its application as a probe for fluorescent polarization assay of PPARδ ligands', Chemical and Pharmaceutical Bulletin, vol. 56, no. 9, pp. 1357-1359. https://doi.org/10.1248/cpb.56.1357

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AU - Kasuga, Jun Ichi

AU - Toyota, Kenji

AU - Hirakawa, Yuko

AU - Oyama, Takuji

AU - Makishima, Makoto

AU - Morikawa, Kosuke

AU - Hashimoto, Yuichi

AU - Miyachi, Hiroyuki

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KW - Fluorescent peroxisome proliferator-activated receptor α/δ co-agonist

KW - Fluorescent polarization

KW - Peroxisome proliferator-activated receptor

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Structure-based design and synthesis of fluorescent PPARα/δ co-agonist and its application as a probe for fluorescent polarization assay of PPARδ ligands

Abstract

Keywords

ASJC Scopus subject areas

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