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[PPARgamma target genes and the molecular mechanism of transcriptional control by PPARgamma]

Makoto Nishizuka1, Masayoshi Imagawa

  • 1Department of Molecular Biology, Graduate School of Pharmaceutical Sciences, Nagoya City University.

Nihon Rinsho. Japanese Journal of Clinical Medicine
|February 18, 2010
PubMed

Insights

Peroxisome proliferator-activated receptor gamma (PPARgamma) agonists, like thiazolidinediones (TZDs), regulate energy, insulin sensitivity, and inflammation. This review details how PPARgamma coactivators and target genes control these vital cellular processes.

Area of Science:

  • Molecular biology
  • Endocrinology
  • Cell biology

Context:

  • Peroxisome proliferator-activated receptor gamma (PPARgamma) is a nuclear receptor crucial for metabolic regulation.
  • PPARgamma activity is modulated by ligand binding, influencing gene expression.
  • Thiazolidinediones (TZDs) are known PPARgamma agonists with diverse physiological effects.

Purpose:

  • To elucidate the transcriptional regulation mechanisms of PPARgamma.
  • To focus on the role of coactivators and target genes in PPARgamma's function.
  • To provide a comprehensive overview of TZD-mediated effects through PPARgamma.

Summary:

  • PPARgamma, a ligand-activated nuclear receptor, controls energy conservation, adipocyte differentiation, and insulin sensitivity.
  • In its inactive state, PPARgamma's transcription is repressed by corepressors like N-CoR/SMRT and histone deacetylases.
  • Ligand binding activates PPARgamma, leading to coactivator recruitment and regulation of target gene expression in various tissues.

Impact:

  • Understanding PPARgamma transcriptional control is key to developing targeted therapies for metabolic and inflammatory diseases.
  • This review highlights the critical role of coactivators and target genes in mediating the pleiotropic effects of PPARgamma agonists.
  • Insights into PPARgamma regulation can inform strategies for managing conditions like diabetes, inflammation, and cancer.

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