Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver

Thiazolidinediones are a class of Peroxisome Proliferator Activated Receptor γ (PPARγ) agonists that reduce insulin resistance in type 2 diabetic patients. Although no detectable hepatic toxicity has been evidenced in animal studies during preclinical trials, these molecules have nevertheless induce...

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Main Authors: Alexandra Rogue, Catherine Spire, Manuel Brun, Nancy Claude, André Guillouzo
Format: Article
Language:English
Published: Wiley 2010-01-01
Series:PPAR Research
Online Access:http://dx.doi.org/10.1155/2010/325183
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author Alexandra Rogue
Catherine Spire
Manuel Brun
Nancy Claude
André Guillouzo
author_facet Alexandra Rogue
Catherine Spire
Manuel Brun
Nancy Claude
André Guillouzo
author_sort Alexandra Rogue
collection DOAJ
description Thiazolidinediones are a class of Peroxisome Proliferator Activated Receptor γ (PPARγ) agonists that reduce insulin resistance in type 2 diabetic patients. Although no detectable hepatic toxicity has been evidenced in animal studies during preclinical trials, these molecules have nevertheless induced hepatic adverse effects in some treated patients. The mechanism(s) of hepatotoxicity remains equivocal. Several studies have been conducted using PCR analysis and microarray technology to identify possible target genes and here we review the data obtained from various in vivo and in vitro experimental models. Although PPARγ is expressed at a much lower level in liver than in adipose tissue, PPARγ agonists exert various PPARγ-dependent effects in liver in addition to PPARγ-independent effects. Differences in effects are dependent on the choice of agonist and experimental conditions in rodent animal studies and in rodent and human liver cell cultures. These effects are much more pronounced in obese and diabetic liver. Moreover, our own recent studies have shown major interindividual variability in the response of primary human hepatocyte populations to troglitazone treatment, supporting the occurrence of hepatotoxicity in only some individuals.
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spelling doaj-art-e9bb426ae4a94c31ba93dac129512ba82025-08-20T03:26:34ZengWileyPPAR Research1687-47571687-47652010-01-01201010.1155/2010/325183325183Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human LiverAlexandra Rogue0Catherine Spire1Manuel Brun2Nancy Claude3André Guillouzo4UMR INSERM U991, Faculté des Sciences Pharmaceutiques et Biologiques, 35043 Rennes, FranceBiologie Servier, 45520 Gidy, FranceInstitut de Recherches Servier, 92150 Suresnes, FranceInstitut de Recherches Servier, 92400 Courbevoie, FranceUMR INSERM U991, Faculté des Sciences Pharmaceutiques et Biologiques, 35043 Rennes, FranceThiazolidinediones are a class of Peroxisome Proliferator Activated Receptor γ (PPARγ) agonists that reduce insulin resistance in type 2 diabetic patients. Although no detectable hepatic toxicity has been evidenced in animal studies during preclinical trials, these molecules have nevertheless induced hepatic adverse effects in some treated patients. The mechanism(s) of hepatotoxicity remains equivocal. Several studies have been conducted using PCR analysis and microarray technology to identify possible target genes and here we review the data obtained from various in vivo and in vitro experimental models. Although PPARγ is expressed at a much lower level in liver than in adipose tissue, PPARγ agonists exert various PPARγ-dependent effects in liver in addition to PPARγ-independent effects. Differences in effects are dependent on the choice of agonist and experimental conditions in rodent animal studies and in rodent and human liver cell cultures. These effects are much more pronounced in obese and diabetic liver. Moreover, our own recent studies have shown major interindividual variability in the response of primary human hepatocyte populations to troglitazone treatment, supporting the occurrence of hepatotoxicity in only some individuals.http://dx.doi.org/10.1155/2010/325183
spellingShingle Alexandra Rogue
Catherine Spire
Manuel Brun
Nancy Claude
André Guillouzo
Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver
PPAR Research
title Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver
title_full Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver
title_fullStr Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver
title_full_unstemmed Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver
title_short Gene Expression Changes Induced by PPAR Gamma Agonists in Animal and Human Liver
title_sort gene expression changes induced by ppar gamma agonists in animal and human liver
url http://dx.doi.org/10.1155/2010/325183
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