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GeneE
50 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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PPARA
peroxisome proliferator activated receptor alpha
Chromosome 22 · 22q13.31
NCBI Gene: 5465Ensembl: ENSG00000186951.18HGNC: HGNC:9232UniProt: F1D8S4
654PubMed Papers
20Diseases
26Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Hub GeneReceptorTranscription Factor
RESEARCH IMPACT
Highly StudiedTrending
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
negative regulation of cytokine production involved in inflammatory responsenegative regulation of reactive oxygen species biosynthetic processnegative regulation of hepatocyte apoptotic processpositive regulation of ATP biosynthetic processtype 2 diabetes mellituscardiovascular diseaseinherited lipid metabolism disorderHypercholesterolemia
✦AI Summary

PPARA (peroxisome proliferator-activated receptor alpha) is a ligand-activated nuclear transcription factor that functions as a master regulator of lipid metabolism and energy homeostasis. As a key executor of fatty acid catabolism, PPARA heterodimerizes with RXRA to activate genes involved in peroxisomal beta-oxidation and hepatic autophagy 1. The receptor is activated by endogenous lipids including palmitoylethanolamide, which signals through PPAR-α-dependent pathways to exert anti-inflammatory effects 2. Mechanistically, PPARA regulates hepatic lipid homeostasis through multiple pathways: it coordinates with PCK1 during fasting to ameliorate non-alcoholic fatty liver disease (NASH) and fibrosis 3, modulates intestinal fatty acid uptake via FABP1 regulation 4, and controls hepatomegaly and liver regeneration through YAP-TEAD signaling activation 5. Additionally, PPARA transcriptionally activates SLC47A1 to protect against ferroptosis-induced cell death 6. Clinically, PPARA activation holds therapeutic potential for multiple diseases. PPARA agonists decrease amyloid-beta pathology and cognitive decline in Alzheimer disease models 1, while PPARA antagonism reduces obesity and NASH progression 4. Evolutionary studies demonstrate that PPARA haplotypes underwent positive selection in Tibetan populations for high-altitude adaptation 7, highlighting its fundamental role in metabolic homeostasis and hypoxia response.

Sources cited
1
PPARα and PCK1 act cooperatively as hepatic executors of fasting response; combined knockdown abolishes beneficial effects against NASH, inflammation, and fibrosis
PMID: 38718791
2
Mas signaling pathway involves PPARα in regulating fatty acid oxidation and hepatocyte protection; study demonstrates PPARα importance in lipid metabolism-related hepatotoxicity
PMID: 36368597
3
Intestinal PPARα regulates FABP1 expression to modulate dietary fatty acid uptake; PPARα antagonism improves obesity and NASH in PPARα-humanized mice
PMID: 35460276
4
Palmitoylethanolamide exerts biological effects through peroxisome proliferator-activated receptor-α (PPAR-α) activation, with PPAR-α-independent pathways also identified
PMID: 33114698
5
PPARA agonists (gemfibrozil, Wy14643) induce autophagy in microglia and glioma cells; PPARA activation decreases amyloid pathology and reverses memory deficits in APP-PSEN1ΔE9 mice
PMID: 30898012
6
PPARα activation induces hepatomegaly and accelerates liver regeneration through YAP-TEAD signaling; effects require hepatocyte-specific PPARα expression
PMID: 34387904
7
PPARA transcriptionally activates SLC47A1; PPARA-SLC47A1 pathway blocks ferroptosis by regulating lipid remodeling and polyunsaturated fatty acid cholesterol ester production
PMID: 36575162
8
PPARA haplotypes underwent positive selection in Tibetan populations and are associated with high-altitude adaptation and decreased hemoglobin phenotype
PMID: 20466884
Disease Associationsⓘ20
type 2 diabetes mellitusOpen Targets
0.62Moderate
cardiovascular diseaseOpen Targets
0.58Moderate
inherited lipid metabolism disorderOpen Targets
0.57Moderate
HypercholesterolemiaOpen Targets
0.57Moderate
familial hyperlipidemiaOpen Targets
0.55Moderate
hyperlipidemiaOpen Targets
0.54Moderate
diabetes mellitusOpen Targets
0.54Moderate
Abnormal circulating lipid concentrationOpen Targets
0.53Moderate
coronary artery diseaseOpen Targets
0.48Moderate
hyperlipoproteinemia type 3Open Targets
0.44Moderate
primary biliary cirrhosisOpen Targets
0.43Moderate
Disorder of lipid metabolismOpen Targets
0.41Moderate
HypertriglyceridemiaOpen Targets
0.40Moderate
hypothyroidismOpen Targets
0.37Weak
non-alcoholic steatohepatitisOpen Targets
0.37Weak
Abdominal painOpen Targets
0.37Weak
biliary liver cirrhosisOpen Targets
0.37Weak
cholangitisOpen Targets
0.37Weak
hyperlipoproteinemiaOpen Targets
0.37Weak
metabolic diseaseOpen Targets
0.35Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets26
ALEGLITAZARPhase III
Peroxisome proliferator-activated receptor alpha agonist
type 2 diabetes mellitus
AVE8134Phase II
Peroxisome proliferator-activated receptor alpha agonist
heart failure
BEZAFIBRATEApproved
Peroxisome proliferator-activated receptor agonist
cardiovascular disease
CHIGLITAZARPhase III
Peroxisome proliferator-activated receptor agonist
type 2 diabetes mellitus
CHOLINE FENOFIBRATEApproved
Peroxisome proliferator-activated receptor alpha agonist
cardiovascular disease
CIPROFIBRATEApproved
Peroxisome proliferator-activated receptor alpha agonist
cardiovascular disease
CLOFIBRATEApproved
Peroxisome proliferator-activated receptor alpha agonist
cardiovascular disease
CP-778875Phase II
Peroxisome proliferator-activated receptor alpha agonist
Disorder of lipid metabolism
DRF-10945Phase I
Peroxisome proliferator-activated receptor alpha agonist
familial hyperlipidemia
ELAFIBRANORApproved
Peroxisome proliferator-activated receptor alpha agonist
biliary liver cirrhosis
FENOFIBRATEApproved
Peroxisome proliferator-activated receptor alpha agonist
type 2 diabetes mellitus
FENOFIBRIC ACIDApproved
Peroxisome proliferator-activated receptor alpha agonist
Hypercholesterolemia
GEMFIBROZILApproved
Peroxisome proliferator-activated receptor alpha agonist
cardiovascular disease
IMIGLITAZARPhase III
Peroxisome proliferator-activated receptor alpha agonist
type 2 diabetes mellitus
INDEGLITAZARPhase II
Peroxisome proliferator-activated receptor agonist
type 2 diabetes mellitus
K-877Phase III
Peroxisome proliferator-activated receptor alpha agonist
Hypertriglyceridemia
LANIFIBRANORPhase III
Peroxisome proliferator-activated receptor agonist
non-alcoholic steatohepatitis
LY-518674Phase II
Peroxisome proliferator-activated receptor alpha agonist
MK-0767Phase III
Peroxisome proliferator-activated receptor alpha agonist
type 2 diabetes mellitus
MURAGLITAZARPhase III
Peroxisome proliferator-activated receptor gamma agonist
type 2 diabetes mellitus
NAVEGLITAZARPhase II
Peroxisome proliferator-activated receptor gamma agonist
PEMAFIBRATEApproved
Peroxisome proliferator-activated receptor alpha agonist
cardiovascular disease
SAROGLITAZARApproved
Peroxisome proliferator-activated receptor alpha agonist
inherited lipid metabolism disorder
SODELGLITAZARPhase II
Peroxisome proliferator-activated receptor agonist
familial hyperlipidemia
TESAGLITAZARPhase III
Peroxisome proliferator-activated receptor alpha agonist
type 1 diabetes mellitus
ZYH7Phase II
Peroxisome proliferator-activated receptor alpha agonist
inherited lipid metabolism disorder
Related Genes
NCOA1Protein interaction100%UCP2Protein interaction100%NCOA2Protein interaction100%NCOR1Protein interaction100%NPAS2Protein interaction99%RXRAProtein interaction98%
Tissue Expression6 tissues
Liver
100%
Heart
82%
Ovary
19%
Brain
15%
Lung
11%
Bone Marrow
4%
Gene Interaction Network
Click a node to explore
PPARANCOA1UCP2NCOA2NCOR1NPAS2RXRA
PROTEIN STRUCTURE
Preparing viewer…
PDB6KAX · 1.23 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.71LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.50 [0.35–0.71]
RankingsWhere PPARA stands among ~20K protein-coding genes
  • #335of 20,598
    Most Researched654 · top 5%
  • #147of 1,025
    FDA-Approved Drug Targets10 · top quartile
  • #5,455of 17,882
    Most Constrained (LOEUF)0.71
Genes detectedPPARA
Sources retrieved50 papers
Response time—
📄 Sources
50▼
1
A 5:2 intermittent fasting regimen ameliorates NASH and fibrosis and blunts HCC development via hepatic PPARα and PCK1.
PMID: 38718791
Cell Metab · 2024
1.00
2
Hepatocyte-specific Mas activation enhances lipophagy and fatty acid oxidation to protect against acetaminophen-induced hepatotoxicity in mice.
PMID: 36368597
J Hepatol · 2023
0.90
3
Cardiomyocyte peroxisome proliferator-activated receptor α prevents septic cardiomyopathy via improving mitochondrial function.
PMID: 37328648
Acta Pharmacol Sin · 2023
0.84
4
Intestinal peroxisome proliferator-activated receptor α-fatty acid-binding protein 1 axis modulates nonalcoholic steatohepatitis.
PMID: 35460276
Hepatology · 2023
0.80
5
Obesity-associated exosomal miRNAs modulate glucose and lipid metabolism in mice.
PMID: 30429322
Proc Natl Acad Sci U S A · 2018
0.80