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PsychedeliaDokholyan Laboratory
TargetNuclear receptors

Peroxisome proliferator-activated receptor alpha

Steroid and other ligand-activated transcription factors.

Measurements
3
Compounds
2
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

PPARA_HUMANPPARAHomo sapiens

Peroxisome proliferator-activated receptor alpha

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

Quoted from UniProt’s FUNCTION annotation for Q07869 (reviewed).

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
RXRA0.9990.8400.9000.986
PPARGC1A0.9990.9590.9000.999
NCOA10.9980.9850.5000.784
NCOR20.9960.9700.5000.778
NCOR10.9910.8330.5000.906
PER20.9890.0910.0000.989
JUN0.9790.0570.0000.979
LPIN10.9740.2920.0000.964
XPR10.9700.0000.0000.970
FABP10.9640.2530.5000.912

Where it sits in the cell

  • Primary cilium
  • Nucleoli fibrillar centeradditional
  • Nuclear bodiesadditional
  • Centriolar satelliteadditional
  • Basal bodyadditional

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

UniProt, curated Nucleus

Expression by cell type

Single cell type RNA, the 4 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Rod photoreceptor cells680.1 nCPM
  • Proximal tubule cells571 nCPM
  • Hepatocytes326.6 nCPM
  • Enterocytes313.3 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.

  • tongue39.7 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.

Brain

cerebral cortex — 4.6 nTPM, from PPARAcerebellum — 1.9 nTPM, from PPARAhippocampal formation — 3.7 nTPM, from PPARAamygdala — 4.9 nTPM, from PPARAhypothalamus — 3.3 nTPM, from PPARAthalamus — no resolved target expressed herebasal ganglia — 5.2 nTPM, from PPARAmedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: retina 16.6, midbrain 5.0, spinal cord 3.8, pituitary gland 2.4.

Body

heart — 26.2 nTPM, from PPARAsmooth muscle — 4.3 nTPM, from PPARAlung — 4.1 nTPM, from PPARAliver — 30.8 nTPM, from PPARAkidney — 20.8 nTPM, from PPARAstomach — 5.5 nTPM, from PPARAduodenum — 17.6 nTPM, from PPARAsmall intestine — 18.1 nTPM, from PPARAcolon — 10.7 nTPM, from PPARAadrenal gland — 6.2 nTPM, from PPARAthyroid gland — 6.9 nTPM, from PPARApancreas — 7.1 nTPM, from PPARAurinary bladder — 4.7 nTPM, from PPARAskeletal muscle — 24.0 nTPM, from PPARAspleen — 4.2 nTPM, from PPARAsalivary gland — 7.1 nTPM, from PPARA
031 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 PPARA 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

  • retina16.6 nTPM
  • basal ganglia5.2 nTPM
  • midbrain5.0 nTPM
  • amygdala4.9 nTPM
  • cerebral cortex4.6 nTPM
  • spinal cord3.8 nTPM
  • hippocampal formation3.7 nTPM
  • hypothalamus3.3 nTPM
  • pituitary gland2.4 nTPM
  • cerebellum1.9 nTPM

Peripheral and autonomic · 16

  • liver30.8 nTPM
  • heart muscle26.2 nTPM
  • skeletal muscle24.0 nTPM
  • kidney20.8 nTPM
  • small intestine18.1 nTPM
  • duodenum17.6 nTPM
  • colon10.7 nTPM
  • pancreas7.1 nTPM
  • salivary gland7.1 nTPM
  • thyroid gland6.9 nTPM
  • adrenal gland6.2 nTPM
  • stomach 15.5 nTPM
  • urinary bladder4.7 nTPM
  • smooth muscle4.3 nTPM
  • spleen4.2 nTPM
  • lung4.1 nTPM

Transcript is not protein. These are RNA levels for PPARA, 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 3

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

TargetClassTypeValue (nM)pXOrganismAssay
Peroxisome proliferator-activated receptor alphaNuclear receptorsEC509,5805.02Homo sapiensCHEMBL5241794
Peroxisome proliferator-activated receptor alphaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291865
Peroxisome proliferator-activated receptor alphaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291864
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