1C. Peroxisome proliferator-activated receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Peroxisome proliferator-activated receptors (PPARs, nomenclature as agreed by NC-IUPHAR Committee on Nuclear Receptors, [17]) 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 [3,17], including 15-deoxy-Δ12,14-PGJ2, prostacyclin (PGI2), many fatty acids and their oxidation products, lysophosphatidic acid (LPA) [16], 13-HODE, 15S-HETE, Paz-PC, azelaoyl-PAF and leukotriene B4 (LTB4). bezafibrate acts as a non-selective agonist for the PPAR family [26]. 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.

Receptors

Peroxisome proliferator-activated receptor-α / NR1C1 Show summary » More detailed page

Peroxisome proliferator-activated receptor-β/δ / NR1C2 Show summary » More detailed page

Peroxisome proliferator-activated receptor-γ / NR1C3 Show summary » More detailed page

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How to cite this family page

Database page citation:

1C. Peroxisome proliferator-activated receptors. Accessed on 24/10/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=86.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: Nuclear Hormone Receptors. Br J Pharmacol. 170: 1652–1675.