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Peroxisome Proliferator-Activated Receptors pp 25–32Cite as

PPAR Ligands

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Abstract

PPARs were originally described as orphan nuclear receptors, but numerous potential endogenous ligand(s) were soon described; however, the real identity of true endogenous PPAR ligand is still very much debated (Varga et al. 2011). All three PPARs are activated by a variety of polyunsaturated long-chain fatty acids and arachidonic acid derivatives (Dreyer et al. 1993; Grimaldi 2007). Because of this, it has been hypothesized that PPARs act as lipid sensors rather than being specific receptors for one particular lipid molecule. This idea suggests an important role for these receptors in adapting the metabolic rates of various tissues to the concentration of dietary lipids (Grimaldi 2007). In addition to these naturally occurring molecules, numerous synthetic ligands of varying selectivity bind to and activate various PPAR subtypes. The lack of strict specificity of ligand binding to PPARs might be attributed, at least in part, to the unusually large ligand-binding pocket in these receptors compared to other more specific nuclear hormone receptors.

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Authors and Affiliations

  1. School of Pharmacy, University of Missouri-Kansas City, Kansas City, MO, USA

    Jihan A. Youssef & Mostafa Z. Badr

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  1. Jihan A. Youssef
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  2. Mostafa Z. Badr
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Youssef, J.A., Badr, M.Z. (2013). PPAR Ligands. In: Peroxisome Proliferator-Activated Receptors. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-420-3_4

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