Search
peroxisome proliferator-activated receptor delta; PPAR-delta; PPAR-beta; nuclear receptor subfamily 1 group C member 2; nuclear hormone receptor 1; NUC1; NUCI (PPARD, NR1C2, PPARB)
Function:
- activated by fatty acids & peroxisome proliferators
- binds to DNA as heterodimer with RXR
- role in embryo implantation [1]
- dUTPase prevents PPAR-RXR heterodimerization
- binds to a promoter element in the gene for acyl-CoA oxidase & activates its transcription, thus controls peroxisomal beta-oxidation pathway of fatty acids
- decreases expression of NPC1L1 once activated by a ligand
- endogenous ligands (activators)
a) saturated fatty acids
1] palmitic acid [16:0] (2+)
2] stearic acid [18:0] (2+)
b) monounsaturated fatty acids
1] palmitoleic acid [16:1] (+)
2] oleic acid [18:1] (2+)
c) polyunsaturated fatty acids
1] linoleic acid [18:2, n-6] (2+)
2] alpha-linolenic acid [18:3, n-3] (+)
3] gamma-linolenic acid [18:3, n-6] (3+)
4] dihomo-gamma-linolenic acid [20:3, n-6] (2+)
5] arachidonic acid [20:4, n-6] (2+)
6] eicosapentaenoic acid [22:5, n-3] (2+)
7] docosahexaenoic acid [22:6, n-3] (2+)
d) eicosanoids
1] PGA1 (2+)
2] PGA2 (+)
3] PGD1 (+)
4] PGD2 (+)
5] PGJ2 (+/-)
Structure:
- belongs to the nuclear hormone receptor family, NR1 subfamily
- contains 1 nuclear receptor DNA-binding domain
Compartment: nucleus
Alternative splicing: named isoforms=2
Expression:
- ubiquitous with maximal levels in placenta & skeletal muscle
- intestine (3+) [1]
Pharmacology:
Exogenous agonists: (peroxisome proliferators) [1]
1) hypolipidemic drugs
a) WY-14-643 (1+)
b) GW2331 (+/-)
g) bezafibrate (3+)
2) non-steroidal anti-inflammatory drugs (NSAIDs)
a) GW2433 (3+)
b) L-165041)
3) other
-> monoethylhexyl phthalate (1+)
Related
retinoid X receptor (RXR)
General
peroxisome proliferator-activated receptor (PPAR)
Properties
SIZE: entity length = 441 aa
MW = 50 kD
COMPARTMENT: cell nucleus
MOTIF: DNA-binding motif
SITE: 71-145
MOTIF: Zn finger C4-type
SITE: 74-94
EFFECTOR-BOUND: Zn+2
Zn finger C4-type
SITE: 111-133
EFFECTOR-BOUND: Zn+2
binding site
SITE: 254-441
FOR-BINDING-OF: ligand
Database Correlations
OMIM 600409
UniProt Q03181
PFAM correlations
Kegg hsa:5467
References
- Corton JC, Anderson SP, Stauber A.
Central role of peroxisome proliferator-activated receptors
in the actions of peroxisome proliferators.
Annu Rev Pharmacol Toxicol. 2000;40:491-518. Review.
PMID: 10836145
- UniProt :accession Q03181
- Wikipedia; peroxisome proliferator-activated receptor entry
http://en.wikipedia.org/wiki/peroxisome_proliferator-activated_receptor