[Nuclear receptors PPAR as a drug target in metabolic disorders]

Postepy Biochem. 2011;57(2):207-14.
[Article in Polish]

Abstract

Nuclear receptors regulate many basic cellular processes and their malfunction can lead to serious consequences including metabolic disorders, obesity and type 2 diabetes. Among many nuclear receptor families, the best known for their therapeutic use are the PPARs. These are key transcription factors determining, proper cellular metabolism of glucose and lipids, tissue sensitivity to insulin, appropriate immune responses including inflammatory processes and finally cell division and differentiation. Currently two types of PPAR activators are in medical use: in the therapy of type 2 diabetes--thiazolidinediones (TZDs), which act via PPARgamma receptors and in the treatment of dyslipidemia-fibrates, which act via PPARalpha receptors. The search for new drugs acting through PPAR mechanism consists in the design of new molecules with tissue specific proprieties, which would selectively bind and modulate the activity of appropriate receptors, thus reducing the number of adverse events typically observed with the use of full agonists. These molecules have been named selective nuclear receptor modulators (SNuRMs).

Publication types

  • English Abstract
  • Review

MeSH terms

  • Diabetes Mellitus, Type 2 / drug therapy
  • Drug Design
  • Humans
  • Metabolic Diseases / drug therapy*
  • Metabolic Diseases / metabolism
  • PPAR alpha / agonists
  • PPAR gamma / agonists
  • Peroxisome Proliferator-Activated Receptors / agonists*
  • Peroxisome Proliferator-Activated Receptors / metabolism
  • Thiazolidinediones / pharmacology

Substances

  • PPAR alpha
  • PPAR gamma
  • Peroxisome Proliferator-Activated Receptors
  • Thiazolidinediones