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.

A novel peroxisome proliferator-activated receptor responsive element-luciferase reporter mouse reveals gender specificity of peroxisome proliferator-activated receptor activity in liver / P. Ciana, A. Biserni, L. Tatangelo, C. Tiveron, AF. Sciarroni, L. Ottobrini, A. Maggi. - In: MOLECULAR ENDOCRINOLOGY. - ISSN 0888-8809. - 21:2(2007 Feb), pp. 388-400.

A novel peroxisome proliferator-activated receptor responsive element-luciferase reporter mouse reveals gender specificity of peroxisome proliferator-activated receptor activity in liver

P. Ciana;BISERNI, ANDREA;L. Ottobrini;A. Maggi
2007-02

Abstract

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.
ALPHA PPAR-ALPHA ; ESTROGEN-RECEPTOR ; GENE-EXPRESSION ; IN-VIVO ; RAT-LIVER ; CLOFIBRIC ACID ; BETA-OXIDATION ; GROWTH-HORMONE ; MALE-MICE ; DIFFERENCE
Settore BIO/14 - Farmacologia
Settore MED/36 - Diagnostica per Immagini e Radioterapia
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/23379
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