TY - JOUR T1 - In Vivo Imaging Reveals Selective Peroxisome Proliferator Activated Receptor Modulator Activity of the Synthetic Ligand 3-(1-(4-Chlorobenzyl)-3-<em>t</em>-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886) JF - Molecular Pharmacology JO - Mol Pharmacol SP - 1434 LP - 1443 DO - 10.1124/mol.107.042689 VL - 73 IS - 5 AU - Andrea Biserni AU - Fabio Giannessi AU - Anna Floriana Sciarroni AU - Ferdinando Maria Milazzo AU - Adriana Maggi AU - Paolo Ciana Y1 - 2008/05/01 UR - http://molpharm.aspetjournals.org/content/73/5/1434.abstract N2 - We report here the finding of a new pharmacological activity of a well known antagonist of peroxisome proliferator-activated receptors (PPARs). PPARs belong to the family of nuclear receptors playing a relevant role in mammalian physiology and are currently believed to represent a major target for the development of innovative drugs for metabolic and inflammatory diseases. In the present study, the application of reporter animal technology was instrumental to obtain the global pharmacological profiling indispensable to unraveling 3-(1-(4-chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)-selective PPAR modulator (SPPARM) activity not underlined by previous traditional, cell-based studies. The results of this study, demonstrating the usefulness of reporter mice, may open new avenues for the development of innovative drugs for cardiovascular, endocrine, neural, and skeletal systems characterized by limited side effects. ER -