title: Detection of bioavailable peroxisome proliferator-activated receptor gamma modulators by a cell-based luciferase reporter system.
abstract: In vitro cell-based reporter assays are a useful tool for the discovery and characterization of nuclear receptor modulators. However, the properties of a given molecule can differ when tested in vitro and in vivo as a result of the molecule's bioavailability. In this work, we describe a methodology that allows the detection of the PPARγ (peroxisome proliferator-activated receptor gamma) agonist bezafibrate in rat serum by an in vitro cell-based reporter assay. This methodology could be adapted to the detection and characterization of bioavailable PPARγ or other nuclear receptor modulators in serum, extending the possibilities of the classical in vitro assays.
authors.affiliation: Centre Tecnològic de Nutrició i Salut-CTNS, TECNIO, Reus 43204, Spain. josep.delbas@ctns.cat
authors.forename: Josep M
authors.initials: JM
authors.lastname: del Bas
authors.forename: Sirle
authors.initials: S
authors.lastname: Laos
authors.forename: Antoni
authors.initials: A
authors.lastname: Caimari
authors.forename: Anna
authors.initials: A
authors.lastname: Crescenti
authors.forename: Lluís
authors.initials: L
authors.lastname: Arola
mesh_terms: D000818:Animals; D001629:Bezafibrate / Q000097:blood* / Q000493:pharmacokinetics; D001682:Biological Availability; D017930:Genes, Reporter; D006367:HeLa Cells; D006801:Humans; D000960:Hypolipidemic Agents / Q000097:blood* / Q000493:pharmacokinetics; D008024:Ligands; D049410:Luciferases, Renilla / Q000032:analysis*; D050506:Mutant Chimeric Proteins / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D047495:PPAR gamma / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D010957:Plasmids; D051381:Rats; D017208:Rats, Wistar; D014162:Transfection
chemical_list: D000960:Hypolipidemic Agents; D008024:Ligands; D050506:Mutant Chimeric Proteins; D047495:PPAR gamma; D049410:Luciferases, Renilla; D001629:Bezafibrate