Peroxisome Proliferator Activated Receptor Alpha (PPARa)

NR1C1; PPAR-A; HPPAR; Nuclear Receptor Subfamily 1 Group C Member 1

SPN	V877
HGNC	9232
MGI	104740
PubMed	22336959
RGD	3369
UniProt	Q07869
Wiki	PPARA

Peroxisome proliferators receptor ligands include hypolipidemic drugs, herbicides, leukotriene antagonists, and plasticizers; this term arises because they induce an increase in the size and number of peroxisomes. Peroxisomes are subcellular organelles found in plants and animals that contain enzymes for respiration and for cholesterol and lipid metabolism. The action of peroxisome proliferators is thought to be mediated via specific receptors, called PPARs, which belong to the steroid hormone receptor superfamily. Three closely related subtypes (alpha, beta/delta, and gamma) have been identified. PPAR-alpha is a nuclear transcription factor. Multiple alternatively spliced transcript variants have been described for this gene, although the full-length nature of only two has been determined.

Reference

"cDNA cloning, chromosomal mapping, and functional characterization of the human peroxisome proliferator activated receptor."
Biochemistry 32:5598-5604(1993) [PubMed] [Europe PMC] [Abstract]

"Human and rat peroxisome proliferator activated receptors (PPARs) demonstrate similar tissue distribution but different responsiveness to PPAR activators."
J. Steroid Biochem. Mol. Biol. 51:157-166(1994) [PubMed] [Europe PMC] [Abstract]

"Peroxisome proliferator-activated receptors: structures and function."
Ann. N. Y. Acad. Sci. 804:252-265(1996) [PubMed] [Europe PMC] [Abstract]

"DNA-binding profiling of human hormone nuclear receptors via fluorescence correlation spectroscopy in a cell-free system."
FEBS Lett. 582:2737-2744(2008) [PubMed] [Europe PMC] [Abstract]

"Optimization of an enzyme-linked immunosorbent assay to screen ligand of Peroxisome proliferator-activated receptor alpha."
Immunopharmacol. Immunotoxicol. 31:459-467(2009) [PubMed] [Europe PMC] [Abstract]

"A genome annotation-driven approach to cloning the human ORFeome."
Genome Biol. 5:R84.1-R84.11(2004) [PubMed] [Europe PMC] [Abstract]

"Complete sequencing and characterization of 21,243 full-length human cDNAs."
Nat. Genet. 36:40-45(2004) [PubMed] [Europe PMC] [Abstract]

"The DNA sequence of human chromosome 22."
Nature 402:489-495(1999) [PubMed] [Europe PMC] [Abstract]

"Peroxisome proliferator-activated receptor mediates cross-talk with thyroid hormone receptor by competition for retinoid X receptor. Possible role of a leucine zipper-like heptad repeat."
J. Biol. Chem. 270:18117-18122(1995) [PubMed] [Europe PMC] [Abstract]

"RAC3, a steroid/nuclear receptor-associated coactivator that is related to SRC-1 and TIF2."
Proc. Natl. Acad. Sci. U.S.A. 94:8479-8484(1997) [PubMed] [Europe PMC] [Abstract]

"Regulation of peroxisome proliferator-activated receptor alpha-induced transactivation by the nuclear orphan receptor TAK1/TR4."
J. Biol. Chem. 273:10948-10957(1998) [PubMed] [Europe PMC] [Abstract]

"Conserved amino acids in the ligand-binding and tau(i) domains of the peroxisome proliferator-activated receptor alpha are necessary for heterodimerization with RXR."
Mol. Cell. Endocrinol. 147:37-47(1999) [PubMed] [Europe PMC] [Abstract]

"Cloning and characterization of RAP250, a nuclear receptor coactivator."
J. Biol. Chem. 275:5308-5317(2000) [PubMed] [Europe PMC] [Abstract]

"Interaction of hepatitis C virus core protein with retinoid X receptor alpha modulates its transcriptional activity."
Hepatology 35:937-946(2002) [PubMed] [Europe PMC] [Abstract]

"Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-alpha."
Nature 425:90-93(2003) [PubMed] [Europe PMC] [Abstract]

"Additional sex comb-like (ASXL) proteins 1 and 2 play opposite roles in adipogenesis via reciprocal regulation of peroxisome proliferator-activated receptor {gamma}."
J. Biol. Chem. 286:1354-1363(2011) [PubMed] [Europe PMC] [Abstract]

"Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors."
Proc. Natl. Acad. Sci. U.S.A. 98:13919-13924(2001) [PubMed] [Europe PMC] [Abstract]

"Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family."
Structure 9:699-706(2001) [PubMed] [Europe PMC] [Abstract]

"Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha."
Nature 415:813-817(2002) [PubMed] [Europe PMC] [Abstract]

"Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists."
Bioorg. Med. Chem. Lett. 17:937-941(2007) [PubMed] [Europe PMC] [Abstract]

"Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents."
J. Med. Chem. 50:685-695(2007) [PubMed] [Europe PMC] [Abstract]

"Adaptability and selectivity of human peroxisome proliferator-activated receptor (PPAR) pan agonists revealed from crystal structures."
Acta Crystallogr. D 65:786-795(2009) [PubMed] [Europe PMC] [Abstract]

"Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes."
Bioorg. Med. Chem. Lett. 19:2468-2473(2009) [PubMed] [Europe PMC] [Abstract]

"Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent."
Proc. Natl. Acad. Sci. U.S.A. 106:262-267(2009) [PubMed] [Europe PMC] [Abstract]