title: Structure-based design and synthesis of fluorescent PPARalpha/delta co-agonist and its application as a probe for fluorescent polarization assay of PPARdelta ligands.
abstract: Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARalpha/delta) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARalpha/delta 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 PPARdelta ligands.
authors.affiliation: Institute of Molecular and Cellular Biosciences, University of Tokyo, Tokyo, Japan.
authors.forename: Yoko
authors.initials: Y
authors.lastname: Araya
authors.forename: Jun-Ichi
authors.initials: J
authors.lastname: Kasuga
authors.forename: Kenji
authors.initials: K
authors.lastname: Toyota
authors.forename: Yuko
authors.initials: Y
authors.lastname: Hirakawa
authors.forename: Takuji
authors.initials: T
authors.lastname: Oyama
authors.forename: Makoto
authors.initials: M
authors.lastname: Makishima
authors.forename: Kosuke
authors.initials: K
authors.lastname: Morikawa
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Hashimoto
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Miyachi