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Selective Modulators of PPAR-gamma Activity: Molecular Aspects Related to Obesity and Side-Effects

Fang Zhang1, Brian E Lavan, Francine M Gregoire

  • 1Department of Biology, Metabolex Inc., 3876 Bay Center Place, Hayward, CA 94545, USA.

PPAR Research
|March 29, 2007
PubMed

Insights

Selective PPAR-gamma modulators (SPPARgammaMs) offer new therapeutic avenues for diabetes by selectively targeting the receptor. These modulators induce distinct cellular responses, paving the way for improved antidiabetic agents.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Pharmacology

Background:

  • Peroxisome proliferator-activated receptor gamma (PPAR-gamma) regulates lipid metabolism and energy balance, playing a role in insulin resistance and obesity.
  • Understanding PPAR-gamma's ligand-binding and cofactor interactions has led to the development of selective modulators (SPPARgammaMs).

Purpose of the Study:

  • To review the mechanism of action and biological effects of recently identified SPPARgammaMs.
  • To highlight the potential of SPPARgammaMs as novel antidiabetic agents.

Main Methods:

  • Review of current literature on PPAR-gamma ligands and modulators.
  • Analysis of molecular mechanisms of SPPARgammaM action, including receptor conformation and cofactor recruitment.
  • Summary of biological effects and therapeutic potential of characterized SPPARgammaMs.

Main Results:

  • SPPARgammaMs exhibit distinct binding modes, leading to varied receptor conformations and differential gene expression.
  • This selectivity allows for tailored biological responses, differentiating them from traditional PPAR-gamma activators.
  • Recently identified SPPARgammaMs include metaglidasen/halofenate, PA-082, and angiotensin receptor antagonists.

Conclusions:

  • SPPARgammaMs represent a promising class of compounds for developing improved antidiabetic therapies.
  • Their selective action offers a potential advantage in managing diabetes with fewer side effects.
  • Further research into SPPARgammaMs could lead to more effective treatments for metabolic disorders.

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