Regulation of gene expression by activation of the peroxisome proliferator-activated receptor gamma with rosiglitazone (BRL 49653) in human adipocytes.
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Rieusset J, Auwerx J, Vidal H
Regulation of gene expression by activation of the peroxisome proliferator-activated receptor gamma with rosiglitazone (BRL 49653) in human adipocytes.
Biochem Biophys Res Commun. 1999 Nov;265(1):265-71.
- PubMed ID
- 10548525 [ View in PubMed]
- Abstract
To better define the mechanism of action of the thiazolidinediones, we incubated freshly isolated human adipocytes with rosiglitazone and investigated the changes in mRNA expression of genes encoding key proteins of adipose tissue functions. Rosiglitazone (10(-6) M, 4 h) increased p85alphaphosphatidylinositol 3-kinase (p85alphaPI-3K) and uncoupling protein-2 mRNA levels and decreased leptin expression. The mRNA levels of insulin receptor, IRS-1, Glut 4, lipoprotein lipase, hormone-sensitive lipase, acylation-stimulating protein, fatty acid transport protein-1, angiotensinogen, plasminogen activator inhibitor-1, and PPARgamma1 and gamma2 were not modified by rosiglitazone treatment. Activation of RXR, the partner of PPARgamma, in the presence of rosiglitazone, increased further p85alphaPI-3K and UCP2 mRNA levels and produced a significant augmentation of Glut 4 expression. Because p85alphaPI-3K is a major component of insulin action, the induction of its expression might explain, at least in part, the insulin-sensitizing effect of the thiazolidinediones.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Rosiglitazone Peroxisome proliferator-activated receptor gamma Protein Humans YesAgonistDetails - Pharmaco-transcriptomics
Drug Drug Groups Gene Gene ID Change Interaction Chromosome Rosiglitazone Approved Investigational LEP 3952 downregulated rosiglitazone results in decreased expression of LEP mRNA 7q32.1 Rosiglitazone Approved Investigational PIK3R1 5295 upregulated rosiglitazone results in increased expression of PIK3R1 mRNA 5q13.1 Rosiglitazone Approved Investigational UCP2 7351 upregulated rosiglitazone results in increased expression of UCP2 mRNA 11q13