Protein / target
Peroxisome proliferator-activated receptor gamma
Protein at a glance
Biological role
Transcription cis-regulatory region 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 that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids.
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Ligand-activated transcription factor that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids (PubMed:16150867, PubMed:20829347, PubMed:23525231, PubMed:8702406, PubMed:8706692, PubMed:9065481). Activated by lipid ligands: binds peroxisome proliferators, such as hypolipidemic drugs, and fatty acids, such as prostaglandin J2 metabolites (PubMed:16150867, PubMed:20829347, PubMed:23525231, PubMed:8702406, PubMed:8706692, PubMed:9065481). Ligand-binding results in a conformational change in the receptor, promoting dissociation of repressors and recruitment of coactivators, and subsequent activation of target gene expression (PubMed:16150867, PubMed:20829347, PubMed:23525231, PubMed:8702406, PubMed:8706692, PubMed:9065481). Specifically binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase (By similarity). Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated pro-inflammatory responses (PubMed:20829347). Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of BMAL1 in the blood vessels (By similarity)
Subcellular location
Domains and Gene Ontology detail (105)Hide
Domains & features
Gene Ontology
- Cchromatin
- Ccytosol
- Cnucleoplasm
- Cnucleus
- Creceptor complex
- CRNA polymerase II transcription regulator complex
- Falpha-actinin binding
- Farachidonate binding
- Fchromatin binding
- FDNA binding
- FDNA binding domain binding
- FDNA-binding transcription activator 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 that forms obligate heterodimers with the retinoic…
- ·nuclear receptor activity
- ·Nuclear Receptor transcription pathway
Lipid & lipoprotein metabolism
- ·Ligand-activated transcription factor that forms obligate heterodimers with the retinoic…
- ·cellular response to low-density lipoprotein particle stimulus
- ·fatty acid metabolic process
- ·long-chain fatty acid transport
Cell migration
- ·negative regulation of blood vessel endothelial cell migration
Transcriptional regulation
- ·Ligand-activated transcription factor that forms obligate heterodimers with the retinoic…
- ·RNA polymerase II transcription regulator complex
- ·DNA-binding transcription activator activity, RNA polymerase II-specific
- ·DNA-binding transcription factor activity
Immune signalling
- ·Ligand-activated transcription factor that forms obligate heterodimers with the retinoic…
- ·beige fat cell differentiation
- ·brown fat cell differentiation
- ·fat cell differentiation
View underlying pathways (8)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.
12 medicines meet Open Targets' target-level approved-medicine definition; the 2 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 gamma agonist
Indicated for Diabetes Mellitus, Diabetes Mellitus, Type 2
Peroxisome proliferator-activated receptor gamma agonist
Indicated for Colitis, Ulcerative, Proctitis
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 PPARG
Gene-level evidence surfaced through the gene PPARGthat 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
40 compounds recorded · 12 approved · 28 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 (8)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 2 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.
- Regulatory approval
Approval: MESALAMINE (ANDA219028)
- New publicationRisk of Pancreatitis With Incretin Therapies Versus Thiazolidinediones in the Veterans Health Administration.
- Safety communication
Drug Safety Update: Rosiglitazone: recommended withdrawal from clinical use
- New publicationMesalamine dose escalation reduces fecal calprotectin in patients with quiescent ulcerative colitis.
- New publicationRecombinant human growth hormone and rosiglitazone for abdominal fat accumulation in HIV-infected patients with insulin resistance: a randomized, double-blind, placebo-controlled, factorial trial.
- New publicationDrospirenone/ethinyl estradiol versus rosiglitazone treatment in overweight adolescents with polycystic ovary syndrome: comparison of metabolic, hormonal, and cardiovascular risk factors.
- New publicationRandomized comparison of the effects of rosiglitazone vs. placebo on peak integrated cardiovascular performance, cardiac structure, and function.
- New publicationRosiglitazone for active ulcerative colitis: a randomized placebo-controlled trial.
- New publicationChronic inflammation in fat plays a crucial role in the development of obesity-related insulin resistance.
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.