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Revisiting PPARγ as a target for the treatment of metabolic disorders

Sun-Sil Choi1, Jiyoung Park1, Jang Hyun Choi1

  • 1Department of Biological Science, School of Life Sciences, Ulsan National Institute of Science and Technology (UNIST), Ulsan 689-798, Korea.

BMB Reports
|August 27, 2014
PubMed

Insights

New strategies are needed to combat rising obesity and metabolic disorders. Targeting post-translational modifications (PTMs) of peroxisome proliferator-activated receptor gamma (PPARγ) offers a promising approach for developing safer anti-diabetic drugs.

Area of Science:

  • Metabolic disorders
  • Endocrinology
  • Pharmacology

Background:

  • Rising obesity rates correlate with increased metabolic disorders like type 2 diabetes and cardiovascular diseases.
  • Peroxisome proliferator-activated receptors (PPARs), particularly PPARγ, are key regulators of energy homeostasis and attractive drug targets.
  • Current PPARγ agonists, thiazolidinediones (TZDs), cause severe side effects, necessitating alternative therapeutic strategies.

Purpose of the Study:

  • To review the role of post-translational modifications (PTMs) in regulating PPARγ activity.
  • To explore PTM modulation as a novel therapeutic strategy for metabolic disorders.
  • To discuss considerations for developing new anti-diabetic drugs targeting PPARγ PTMs.

Main Methods:

  • Literature review of studies on PPARγ, PTMs, and metabolic disorders.
  • Analysis of existing data on TZD side effects and alternative therapeutic approaches.
  • Discussion of potential drug development pathways targeting PPARγ PTMs.

Main Results:

  • PPARγ activity can be modulated through various PTMs.
  • Targeting PPARγ PTMs presents a potential avenue for developing anti-diabetic treatments with improved safety profiles.
  • Understanding PTM regulation is crucial for designing effective and safe PPARγ-modulating drugs.

Conclusions:

  • PPARγ PTMs offer a promising strategy to overcome the limitations of current TZD therapies for metabolic disorders.
  • Further research into PPARγ PTM regulation is essential for the development of novel anti-diabetic drugs.
  • Modulating PPARγ PTMs could lead to safer and more effective treatments for obesity-related metabolic diseases.

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