Protein / target
Peroxisome proliferator-activated receptor alpha
Protein at a glance
Biological role
Mitogen-activated protein kinase kinase kinase binding
Strongest disease association
Diabetes Mellitus, Type 2
Therapeutic position
Established drug target
Research activity
Emerging research
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Ligand-activated transcription factor.
View complete UniProt function annotationHide complete annotation
Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as a transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2
Subcellular location
Domains and Gene Ontology detail (73)Hide
Domains & features
Gene Ontology
- Cchromatin
- Cfibrillar center
- Cnuclear body
- Cnucleoplasm
- Cnucleus
- CRNA polymerase II transcription regulator complex
- FDNA binding
- FDNA-binding transcription activator activity
- FDNA-binding transcription activator activity, RNA polymerase II-specific
- FDNA-binding transcription factor activity
- FDNA-binding transcription factor activity, RNA polymerase II-specific
- FDNA-binding transcription repressor activity, RNA polymerase II-specific
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Nuclear receptor signalling
- ·Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by t…
- ·nuclear receptor activity
- ·Nuclear Receptor transcription pathway
Lipid & lipoprotein metabolism
- ·Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by t…
- ·fatty acid metabolic process
- ·lipoprotein metabolic process
- ·negative regulation of cholesterol storage
Transcriptional regulation
- ·Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by t…
- ·RNA polymerase II transcription regulator complex
- ·DNA-binding transcription activator activity
- ·DNA-binding transcription activator activity, RNA polymerase II-specific
Kinase signalling
- ·mitogen-activated protein kinase kinase kinase binding
- ·negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
Immune signalling
- ·negative regulation of cytokine production involved in inflammatory response
- ·negative regulation of inflammatory response
View underlying pathways (13)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
Broader indication categories (1)Hide
Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.
10 medicines meet Open Targets' target-level approved-medicine definition; the 3 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Peroxisome proliferator-activated receptor alpha agonist
Indicated for Diabetes Mellitus, Diabetes Mellitus, Type 2, Dyslipidemias, Hypercholesterolemia
Peroxisome proliferator-activated receptor alpha agonist
Indicated for Abdominal Pain, Coronary Disease, Cardiovascular Diseases
Peroxisome proliferator-activated receptor alpha agonist
Indicated for Cholangitis
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene PPARA
Gene-level evidence surfaced through the gene PPARAthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
View evidence synthesis (5)Hide
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.
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Drug development
27 compounds recorded · 10 approved · 17 in clinical development
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Protein degraders — Emerging
View underlying tractability evidence (7)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 3 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: FENOFIBRATE (ANDA211122)
- Label change
Label change: ELAFIBRANOR (NDA218860)
- Label change
Label change: FENOFIBRATE (ANDA204475)
- Supplemental approval
Supplemental approval: FENOFIBRATE (ANDA208476)
- Product recall
Recall (Class II): FENOFIBRATE
- Supplemental approval
Supplemental approval: FENOFIBRATE (ANDA208476)
- Regulatory approval
Approval: Iqirvo (EMA)
- Regulatory approval
Approval: ELAFIBRANOR (NDA218860)
- New publicationNeuroprotective effects of gemfibrozil in neurological disorders: Focus on inflammation and molecular mechanisms.
- New publicationThe Novel Role of PPAR Alpha in the Brain: Promising Target in Therapy of Alzheimer's Disease and Other Neurodegenerative Disorders.
- New publicationFenofibrate lowers blood pressure in salt-sensitive but not salt-resistant hypertension.
- New publicationGemfibrozil for the secondary prevention of coronary heart disease in men with low levels of high-density lipoprotein cholesterol. Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial Study Group.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.
Research activity
Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.
Most cited
Recent
Europe PMC papers linked directly to this protein.
Related family literature
Papers about “Peroxisome Proliferator-Activated Receptors” — a broader family this protein belongs to. Shown as context; not counted as papers specifically about this protein.
via Peroxisome Proliferator-Activated Receptors
via Peroxisome Proliferator-Activated Receptors
via Peroxisome Proliferator-Activated Receptors
via Peroxisome Proliferator-Activated Receptors
Europe PMC literature, reached through curated HGNC family membership. Membership is a taxonomic relationship — it does not imply this protein participates in every mechanism these papers discuss.