[Design and synthesis of peroxisome proliferator-activated receptor (PPAR) delta agonists and its implication to the driving force to elicit PPAR delta selectivity].

@article{Kasuga2009DesignAS,
  title={[Design and synthesis of peroxisome proliferator-activated receptor (PPAR) delta agonists and its implication to the driving force to elicit PPAR delta selectivity].},
  author={Jun-ichi Kasuga and Takuji Oyama and Izumi Nakagome and Atsushi Aoyama and Kumiko Sako and Makoto Makishima and Shuichi Hirono and Kosuke Morikawa and Yuichi Hashimoto and Hiroyuki Miyachi},
  journal={Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan},
  year={2009},
  volume={129 6},
  pages={
          709-18
        }
}
A series of 3-(4-alkoxypheny)propanoic acid derivatives was prepared as candidate peroxisome proliferator-activated receptor (PPAR) delta-selective agonists, based on our previously discovered potent human PPARalpha/delta dual agonist TIPP-401 as a lead compound. Structure-activity relationship studies clearly indicated the importance of the chain length of the alkoxy group at the 4-position, and the n-butoxy compound exhibited the most potent PPARdelta transactivation activity and highest… 
2 Citations
Crystal Structures of the Human Peroxisome Proliferator-Activated Receptor (PPAR)α Ligand-Binding Domain in Complexes with a Series of Phenylpropanoic Acid Derivatives Generated by a Ligand-Exchange Soaking Method.
TLDR
The "ligand-exchange soaking method," which crystallizes the recombinant PPARα ligand-binding domain (LBD) as a complex with intrinsic fatty acids derived from an expression host Escherichia (E.) coli and thereafter replaces them with other higher-affinity ligands by soaking, is developed.

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