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Expert Opin Ther Targets. 2012 Feb;16(2):209-23. doi: 10.1517/14728222.2012.658370. Epub 2012 Jan 27.

Targeting PPARβ/δ for the treatment of type 2 diabetes mellitus.

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1
University of Barcelona, Department of Pharmacology and Therapeutic Chemistry, Barcelona, Spain.

Abstract

INTRODUCTION:

The nuclear receptors Peroxisome Proliferator-Activated Receptors (PPAR)α and PPARγ are therapeutic targets for hypertriglyceridemia and insulin resistance, respectively. Evidence is now emerging that the PPARβ/δ isotype is a potential pharmacological target for the treatment of insulin resistance and type 2 diabetes mellitus.

AREAS COVERED:

In this review, the capacity of PPARβ/δ to prevent the development of insulin resistance and type 2 diabetes mellitus is discussed. Special emphasis is placed on preclinical studies and the molecular mechanisms responsible for its actions in the main cell types involved in these pathologies: adipocytes, β-cells, skeletal muscle cells and hepatocytes.

EXPERT OPINION:

While several concerns remain for the development of PPARβ/δ agonists, these drugs have demonstrated their efficacy in the treatment of insulin resistance and type 2 diabetes mellitus in preclinical studies, as well as in a few short clinical studies in humans. Although this data is promising, additional studies must be performed to confirm the efficacy and safety of these drugs in the treatment of type 2 diabetes mellitus.

PMID:
22280315
DOI:
10.1517/14728222.2012.658370
[Indexed for MEDLINE]

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