Structure-based design and synthesis of fluorescent PPARalpha/delta co-agonist and its application as a probe for fluorescent polarization assay of PPARdelta ligands.
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.
Araya
Yoko
Y
Institute of Molecular and Cellular Biosciences, University of Tokyo, Tokyo, Japan.
Kasuga
Jun-Ichi
J
Toyota
Kenji
K
Hirakawa
Yuko
Y
Oyama
Takuji
T
Makishima
Makoto
M
Morikawa
Kosuke
K
Hashimoto
Yuichi
Y
Miyachi
Hiroyuki
H