Titre
Molecular basis of selective PPARgamma modulation for the treatment of Type 2 diabetes.
Type
synthèse (review)
Institution
UNIL/CHUV/Unisanté + institutions partenaires
Auteur(s)
Gelman, L.
Auteure/Auteur
Feige, J.N.
Auteure/Auteur
Desvergne, B.
Auteure/Auteur
Liens vers les personnes
Liens vers les unités
ISSN
1388-1981
Statut éditorial
Publié
Date de publication
2007
Volume
1771
Numéro
8
Première page
1094
Dernière page/numéro d’article
1107
Peer-reviewed
Oui
Langue
anglais
Résumé
Peroxisome proliferator-activated receptors (PPARs) (alpha, beta/delta and gamma) are lipid sensors capable of adapting gene expression to integrate various lipid signals. As such, PPARs are also very important pharmaceutical targets, and specific synthetic ligands exist for the different isotypes and are either currently used or hold promises in the treatment of major metabolic disorders. In particular, compounds of the class of the thiazolinediones (TZDs) are PPARgamma agonists and potent insulin-sensitizers. The specific but still broad expression patterns of PPARgamma, as well as its implication in numerous pathways, constitutes also a disadvantage regarding drug administration, since this potentially increases the chance to generate side-effects through the activation of the receptor in tissues or cells not affected by the disease. Actually, numerous side effects associated with the administration of TZDs have been reported. Today, a new generation of PPARgamma modulators is being actively developed to activate the receptor more specifically, in a cell and time-dependent manner, in order to induce a specific subset of target genes only and modulate a restricted number of metabolic pathways. We will discuss here why and how the development of such selective PPARgamma modulators is possible, and summarize the results obtained with the published molecules.
PID Serval
serval:BIB_9B36E01D61D4
PMID
Date de création
2008-01-24T14:26:49.313Z
Date de création dans IRIS
2025-05-21T02:45:17Z