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2007, Number S4

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Arch Cardiol Mex 2007; 77 (S4)

PPARs, metabolic syndrome and cardiac diseases

Carvajal K, Hernández-Esquivel ML, Moreno-Sánchez R

Language: Spanish
References: 44
Page: 66-76
PDF size: 242.08 Kb.


ABSTRACT

The nuclear receptor PPARs (peroxisomal proliferators-activated receptors) are transcription factors activated by natural and synthetic ligands. Three different isoforms of PPARs have been described, PPARα, PPARβ/δ, and PPARγ. PPARs isoforms are tissue-dependent expressed and they regulate the gene expression of proteins involved in glucose and lipid metabolism. Selective pharmacological activation of these isoforms has revealed their role in cellular physiology. Nowadays, two kinds of PPARs agonists are currently used in the clinical practice, the fibrate hypolipidemic drugs, used in the treatment of dyslipidemia, are synthetic ligands for PPARα, whereas thiazolidinediones or glitazones have PPARγ selectivity and are used as hypoglycemic agents. The main cellular effect of PPAR activation lies on fatty acid oxidation and mobilization (PPARα) as well as they act as insulin sensitizers on peripheral tissues (PPARγ). In addition to these beneficial effects of PPARs, it has also been demonstrated that PPARs activation can prevent cardiac dysfunction in diabetic patients as well as the anti-inflammatory processes developed in many diseases. Recent development of PPARβ/δ and hybrid PPARs α and γ agonists, and their clinical trials are giving promising outcomes in the therapeutics of metabolic syndrome, diabetes and cardiac diseases.


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