Peroxisome proliferator-activated receptors (PPARs, nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [1,16]) are nuclear hormone receptors of the NR1C family, with diverse roles regulating lipid homeostasis, cellular differentiation, proliferation and the immune response. PPARs have many potential endogenous agonists [3,16], including 15-deoxy-Δ^12,14-PGJ₂, prostacyclin (PGI₂), many fatty acids and their oxidation products, lysophosphatidic acid (LPA) [15], 13-HODE, 15S-HETE, Paz-PC, azelaoyl-PAF and leukotriene B4 (LTB₄). Bezafibrate acts as a non-selective agonist for the PPAR family [24]. These receptors also bind hypolipidaemic drugs (PPARα) and anti-diabetic thiazolidinediones (PPARγ), as well as many non-steroidal anti-inflammatory drugs, such as sulindac and indomethacin. Once activated by a ligand, the receptor forms a heterodimer with members of the retinoid X receptor family and can act as a transcription factor. Although radioligand binding assays have been described for all three receptors, the radioligands are not commercially available. Commonly, receptor occupancy studies are conducted using fluorescent ligands and truncated forms of the receptor limited to the ligand binding domain.

As with the estrogen receptor antagonists, many agents show tissue-selective efficacy (e.g. [2,17,19]). Agonists with mixed activity at PPARα and PPARγ have also been described (e.g [7,9,26]).

* Key recommended reading is highlighted with an asterisk

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