Rational drug design and PPAR Agonists

Sep 29, 2005Current diabetes reports

Designing Drugs that Activate PPAR Proteins

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Abstract

Thiazolidinediones (TZDs) are a new class of oral drugs that reduce insulin resistance, which is associated with type 2 diabetes and metabolic syndrome.

Insulin resistance is a key abnormality linked to type 2 diabetes and metabolic syndrome.
TZDs act on specific receptors to decrease insulin resistance.
Current recommendations limit TZD use primarily to diabetes treatment.
A better understanding of metabolic syndrome may lead to expanded TZD use for related disorders.
The article reviews TZD mechanisms and discusses potential future antidiabetic drugs.

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Insulin resistance is a characteristic biological abnormality associated with type 2 diabetes, and is a key component of the metabolic syndrome, a condition in which an altered glucose control is associated with dyslipidemia, hypertension, and obesity. Thiazolidinediones (TZDs), a new class of oral drugs used for the treatment of type 2 diabetes, reduce insulin resistance via an action on peroxisome proliferator-activated receptors. Although the current use of TZDs is largely limited to the treatment of patients with diabetes, as recommended in the package insert, it is foreseeable that as the metabolic syndrome becomes a better understood clinical condition their use may be extended to the treatment of this cluster of disorders. The aim of the present article is to review the mechanism of action of TZDs, discuss the rationale for their use in the clinical setting, and provide an update on novel pharmacologic agents that, although not yet available for the treatment of diabetes, are likely to further enrich the repertoire of antidiabetic drugs in the very near future.

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Rational drug design and PPAR Agonists

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