Evaluation of synthetic sphingolipid analogs as ligands for peroxisome proliferator-activated receptors.
In this Letter, we assessed newly synthesized sphingolipid analogs as ligands for peroxisome proliferator-activated receptor (PPAR)alpha, PPARbeta or PPARgamma, using a dual-luciferase reporter system. We tested 640 sphingolipid analogs for ligand activity. As a result, seven types: A9, B9, C9, C50, F66, G66 and H66, were found to show agonistic activities for PPARs.
Tsuji
Kiyomi
K
Laboratory of Biomembrane and Biofunctional Chemistry, Faculty of Advanced Life Science, Hokkaido University, Nishi 11, Kita 21, Kita-ku, Sapporo 001-0021, Japan.
Satoh
Shigeru
S
Mitsutake
Susumu
S
Murakami
Itsuo
I
Park
Jeong-Ju
JJ
Li
Qian
Q
Chang
Young-Tae
YT
Chung
Sung-Kee
SK
Igarashi
Yasuyuki
Y
D000818:Animals; D002518:Ceramides / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D017930:Genes, Reporter; D008024:Ligands; D008156:Luciferases / Q000378:metabolism; D051379:Mice; D041681:NIH 3T3 Cells; D047492:Peroxisome Proliferator-Activated Receptors / Q000378:metabolism*; D010957:Plasmids / Q000378:metabolism; D013107:Sphingolipids / Q000138:chemical synthesis* / Q000494:pharmacology; D014158:Transcription, Genetic; D015533:Transcriptional Activation
D002518:Ceramides; D008024:Ligands; D047492:Peroxisome Proliferator-Activated Receptors; D013107:Sphingolipids; D008156:Luciferases