Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: effect of introduction of fluorine at the linker part.
We developed a potent peroxisome proliferator-activated receptor pan agonist (a candidate drug for treatment of altered metabolic homeostasis) by introducing fluorine atoms at appropriate position(s) of the known phenylpropionic acid-type pan agonist TIPP-703.
Kasuga
Jun-ichi
J
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. jk817@msn.com
Oyama
Takuji
T
Hirakawa
Yuko
Y
Makishima
Makoto
M
Morikawa
Kosuke
K
Hashimoto
Yuichi
Y
Miyachi
Hiroyuki
H
D002087:Butyrates / Q000737:chemistry; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005461:Fluorine / Q000737:chemistry*; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000737:chemistry; D008956:Models, Chemical; D008968:Molecular Conformation; D047494:PPAR delta / Q000819:agonists; D047495:PPAR gamma / Q000819:agonists; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists*; D010666:Phenylpropionates / Q000737:chemistry*; D013329:Structure-Activity Relationship; D015533:Transcriptional Activation
D002087:Butyrates; D006845:Hydrocarbons, Fluorinated; D047494:PPAR delta; D047495:PPAR gamma; D047492:Peroxisome Proliferator-Activated Receptors; D010666:Phenylpropionates; C522376:TIPP-401; D005461:Fluorine