Postepy biochemiiSep 15, 2011

Using PPAR Proteins as Drug Targets for Metabolic Disorders

Updated Apr 3, 2026

Abstract

Nuclear receptors, particularly PPARs, are crucial for regulating cellular metabolism and may contribute to serious conditions like metabolic disorders.

Malfunction of nuclear receptors can lead to metabolic disorders, obesity, and type 2 diabetes.
PPARs are key transcription factors that influence glucose and lipid metabolism, insulin sensitivity, immune responses, and cell differentiation.
Two types of PPAR activators are currently used in medicine: thiazolidinediones (TZDs) for type 2 diabetes and fibrates for dyslipidemia.
Research is ongoing to develop selective nuclear receptor modulators (SNuRMs) that could provide tissue-specific effects and reduce adverse events from full agonists.

Simplified

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).

Using PPAR Proteins as Drug Targets for Metabolic Disorders

Abstract

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