PPARA binds fibrates

Stable Identifier
Reaction [transition]
Homo sapiens
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The peroxisome proliferator-activated receptor alpha (PPARA) is a nuclear ligand-activated transcription factor that is a key regulator of fatty acid oxidation in the liver. Target genes of PPARA participate in fatty acid transport, fatty acid oxidation, triglyceride clearance, lipoprotein production, and cholesterol homeostasis. Its activation mediates lipid, glucose and amino acid homeostasis.

Fibrate drugs are derivatives of fibric acid which act as PPARA agonists and are widely used to lower triglycerides, LDL-cholesterol, total-cholesterol and apolipoprotein C3 (Grundy & Vega 1987, Clavey et al. 1999) while increasing HDL-cholesterol concentrations in serum. They are used to treat hypercholesterolemia, dyslipidemia and hypertriglyceridemia (Katsiki et al. 2013, Laufs et al. 2020). Fibrate drugs include gemfibrozil (De Filippis et al. 2011), bezafibrate (Inoue et al. 2002), cipofibrate (Quang et al. 2012), clofibrate (Henke et al. 1998) and fenofibrate (Caldwell 1989).
Literature References
PubMed ID Title Journal Year
10494028 Cell culture conditions determine apolipoprotein CIII secretion and regulation by fibrates in human hepatoma HepG2 cells

Copin, C, Staels, B, Fruchart, J, Dallongeville, J, Mariotte, MC, Baugé, E, Clavey, V, Fruchart, JC, Chinetti, G

Cell Physiol Biochem 1999
9836620 N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents

Collins, JL, Brackeen, MF, Kliewer, SA, Lehmann, JM, Blanchard, SG, Brown, KK, Leesnitzer, LM, Henke, BR, Hull-Ryde, EA, Miller, JF, Kaldor, I, Willson, TM, Szewczyk, JR, Orband-Miller, LA, Cobb, JE, Harrington, WW, Oliver, W, Mook, RA, Plunket, KD, Noble, SA, Lenhard, JM, Parks, DJ, Lake, DH, Hashim, MA

J Med Chem 1998
11779144 Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB

Kusama, H, Aoyagi, S, Awata, T, Hayashi, K, Katayama, S, Mastunaga, T, Tazawa, S, Komoda, T, Itoh, F, Akahane, M, Inoue, I

Biochem Biophys Res Commun 2002
21889235 Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism

De Filippis, B, Maccallini, C, Fantacuzzi, M, Ammazzalorso, A, Giampietro, L, Giancristofaro, A, Petruzzelli, M, Amoroso, R, D'Angelo, A

Eur J Med Chem 2011
22381047 Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii

Tai, BH, Thao, NP, Quang, TH, Song, SB, Ngan, NT, Kiem, PV, Kim, YH, Minh, CV

Bioorg Med Chem Lett 2012
2713875 The biochemical pharmacology of fenofibrate

Caldwell, J

Cardiology 1989
Orthologous Events
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