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TargetNuclear receptors

Peroxisome proliferator-activated receptor gamma

Steroid and other ligand-activated transcription factors.

Measurements
14
Compounds
8
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

PPARG_HUMANPPARGHomo sapiens

Peroxisome proliferator-activated receptor gamma

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 acids16150867,20829347,23525231,8702406,8706692,9065481. Activated by lipid ligands: binds peroxisome proliferators, such as hypolipidemic drugs, and fatty acids, such as prostaglandin J2 metabolites16150867,20829347,23525231,8702406,8706692,9065481. Ligand-binding results in a conformational change in the receptor, promoting dissociation of repressors and recruitment of coactivators, and subsequent activation of target gene expression16150867,20829347,23525231,8702406,8706692,9065481. 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 responses20829347. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of BMAL1 in the blood vessels (By similarity)
Nuclear receptor that acts as the key factor controlling the development of adipocytes (By similarity). Specifically activated by 15-deoxy-delta12,14-prostaglandin J2 ligand during early adipogenesis, driving differentiation of all types of adipocytes (white, beige and brown) (By similarity). Acts together with retinoic acid receptor RXRA, forming the ARF6 complex, which acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer (By similarity). Following recruitment of TLE3, promotes differentiation of white adipocytes (By similarity). Following recruitment of PRDM16, promotes differentiation of myoblastic precursors into brown adipose cells (BAT), which are specialized in dissipating energy in the form of heat in response to cold or excess feeding (By similarity). Also mediates diffentiation of white adipocytes into beige adipocytes by mediating recruitment of PRDM16 (By similarity)
(Microbial infection) Upon treatment with M.tuberculosis or its lipoprotein LpqH, phosphorylation of MAPK p38 and IL-6 production are modulated, probably via this protein

Quoted from UniProt’s FUNCTION annotation for P37231 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
PPARGC1A0.9990.9920.5000.999
NCOR10.9990.9840.5000.986
NCOR20.9990.9840.5000.920
RXRA0.9990.9990.9000.987
MED10.9990.9860.5000.961
NCOA10.9990.9920.5000.907
CREBBP0.9980.9820.5000.886
NCOA20.9980.9650.5000.902
RELA0.9980.8340.7500.976
SIRT10.9980.3450.9000.981

Where it sits in the cell

  • Nucleoplasm
  • Vesicles

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Nucleus · Cytoplasm

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Urothelial cells4,300.8 nCPM
  • Adipocytes2,246.8 nCPM
  • Prostatic hillock cells990.2 nCPM
  • Papillary tip epithelial cells818.5 nCPM
  • Prostatic club cells766.8 nCPM
  • Foveolar cells753.3 nCPM
  • Extravillous trophoblasts539.7 nCPM
  • Colonocytes505.7 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • adipose tissue153.2 nTPM
  • breast83.9 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

063 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of PPARG transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 10

  • hippocampal formation3.0 nTPM
  • cerebral cortex2.9 nTPM
  • cerebellum2.8 nTPM
  • amygdala2.5 nTPM
  • basal ganglia2.3 nTPM
  • spinal cord2.2 nTPM
  • hypothalamus1.5 nTPM
  • midbrain1.5 nTPM
  • retina0.6 nTPM
  • pituitary gland0.5 nTPM

Peripheral and autonomic · 16

  • urinary bladder63.1 nTPM
  • colon47.8 nTPM
  • stomach 133.1 nTPM
  • lung26.7 nTPM
  • duodenum21.5 nTPM
  • liver16.2 nTPM
  • kidney14.7 nTPM
  • heart muscle13.9 nTPM
  • thyroid gland13.6 nTPM
  • small intestine13.4 nTPM
  • spleen11.0 nTPM
  • smooth muscle8.0 nTPM
  • salivary gland5.5 nTPM
  • skeletal muscle5.0 nTPM
  • adrenal gland3.8 nTPM
  • pancreas2.4 nTPM

Transcript is not protein. These are RNA levels for PPARG, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 14

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291867
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291867
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291867
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291867
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291867
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291866
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291866
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291866
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291866
Peroxisome proliferator-activated receptor gammaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291866
Peroxisome proliferator-activated receptor gammaNuclear receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4618125
Peroxisome proliferator-activated receptor gammaNuclear receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4618125
Peroxisome proliferator-activated receptor gammaNuclear receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4618125
Peroxisome proliferator-activated receptor gammaNuclear receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4618125