The Therapeutic Role of Xenobiotic Nuclear Receptors Against Metabolic Syndrome

Curr Drug Metab. 2019;20(1):15-22. doi: 10.2174/1389200219666180611083155.

Abstract

Background: Diabetes, with an increased prevalence and various progressive complications, has become a significant global health challenge. The concrete mechanisms responsible for the development of diabetes still remain incompletely unknown, although substantial researches have been conducted to search for the effective therapeutic targets. This review aims to reveal the novel roles of Xenobiotic Nuclear Receptors (XNRs), including the Peroxisome Proliferator-Activated Receptor (PPAR), the Farnesoid X Receptor (FXR), the Liver X Receptor (LXR), the Pregnane X Receptor (PXR) and the Constitutive Androstane Receptor (CAR), in the development of diabetes and provide potential strategies for research and treatment of metabolic diseases.

Methods: We retrieved a large number of original data about these five XNRs and organized to focus on their recently discovered functions in diabetes and its complications.

Results: Increasing evidences have suggested that PPAR, FXR, LXR ,PXR and CAR are involved in the development of diabetes and its complications through different mechanisms, including the regulation of glucose and lipid metabolism, insulin and inflammation response and related others.

Conclusion: PPAR, FXR, LXR, PXR, and CAR, as the receptors for numerous natural or synthetic compounds, may be the most effective therapeutic targets in the treatment of metabolic diseases.

Keywords: Constitutive Androstane Receptor (CAR); Farnesoid X Receptor (FXR); Liver X Receptor (LXR); Peroxisome Proliferator-Activated Receptor (PPAR); Pregnane X Receptor (PXR); Xenobiotic Nuclear Receptors (XNRs); diabetes..

Publication types

  • Review

MeSH terms

  • Animals
  • Constitutive Androstane Receptor
  • Humans
  • Liver X Receptors / metabolism
  • Metabolic Syndrome / metabolism*
  • Metabolic Syndrome / pathology
  • Metabolic Syndrome / therapy*
  • Molecular Targeted Therapy
  • Peroxisome Proliferator-Activated Receptors / agonists
  • Peroxisome Proliferator-Activated Receptors / metabolism
  • Pregnane X Receptor / metabolism
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Xenobiotics / metabolism*

Substances

  • Constitutive Androstane Receptor
  • Liver X Receptors
  • Peroxisome Proliferator-Activated Receptors
  • Pregnane X Receptor
  • Receptors, Cytoplasmic and Nuclear
  • Xenobiotics
  • farnesoid X-activated receptor