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First published on February 21, 2008; DOI: 10.1124/mol.107.042689

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Received for publication October 18, 2007.
Revised February 13, 2008.
Accepted for publication February 21, 2008.

IN VIVO IMAGING REVEALS SELECTIVE PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR MODULATOR (SPPARM) ACTIVITY OF THE SYNTHETIC LIGAND MK-886

andrea biserni 1, fabio giannessi 2, anna floriana sciarroni 2, ferdinando maria milazzo 2, adriana maggi 1*, paolo ciana 1

1 Center of Excellence on Neurodegenerative Diseases, Dep. of Pharm. Sci., University of Milan. 2 Sigma-tau Industrie Farmaceutiche Riunite S.p.A.

* Address correspondence to: E-mail: adriana.maggi{at}unimi.it

Abstract

We here report 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 (NRs) 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 unravel MK-886 Selective Peroxisome Proliferator Activated Receptor Modulator (SPPARM) activity not underlined by previous traditional, cell-based studies. The results of the 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.


Key words: PPARs, DNA binding sites, Regulation of gene expression, Cholesterol metabolism/lipoproteins




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