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PsychedeliaDokholyan Laboratory
TargetEnzymes

Prostaglandin G/H synthase 1

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
35
Compounds
14
Binding constants
7
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

PGH1_HUMANPTGS1Homo sapiens

Prostaglandin G/H synthase 1

Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons7947975. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells (Probable). Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity)

Quoted from UniProt’s FUNCTION annotation for P23219 (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
PTGIS0.9730.3220.9000.633
PTGES0.9730.0000.9000.741
ALOX50.9700.0000.9000.692
PTGES20.9620.0000.9000.635
ALOX150.9600.0460.9000.607
ALOX120.9600.0000.9000.544
PTGES30.9560.0000.9000.579
PTGDS0.9490.0000.9000.510
HPGDS0.9460.0000.9000.462
PTGS20.9460.2920.9000.192

Where it sits in the cell

  • Golgi apparatus
  • Vesicles

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

UniProt, curated Microsome membrane · Endoplasmic reticulum membrane

Expression by cell type

Single cell type RNA, the 6 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Platelets1,502.3 nCPM
  • Tuft cells795.4 nCPM
  • Endometrial luminal cells498.1 nCPM
  • Megakaryocytes284.4 nCPM
  • Mast cells219.5 nCPM
  • Smooth muscle cells174 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.

  • urinary bladder227.5 nTPM
  • skin 1144 nTPM
  • intestine102 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 — 2.7 nTPM, from PTGS1cerebellum — 0.3 nTPM, from PTGS1hippocampal formation — 2.5 nTPM, from PTGS1amygdala — 1.4 nTPM, from PTGS1hypothalamus — 2.1 nTPM, from PTGS1thalamus — no resolved target expressed herebasal ganglia — 1.1 nTPM, from PTGS1medulla 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: spinal cord 4.1, pituitary gland 3.8, midbrain 2.8, retina 0.7.

Body

heart — 12.0 nTPM, from PTGS1smooth muscle — 15.0 nTPM, from PTGS1lung — 10.6 nTPM, from PTGS1liver — 2.8 nTPM, from PTGS1kidney — 8.7 nTPM, from PTGS1stomach — 18.8 nTPM, from PTGS1duodenum — 10.2 nTPM, from PTGS1small intestine — 17.4 nTPM, from PTGS1colon — 102.0 nTPM, from PTGS1adrenal gland — 2.8 nTPM, from PTGS1thyroid gland — 2.7 nTPM, from PTGS1pancreas — 1.7 nTPM, from PTGS1urinary bladder — 227.5 nTPM, from PTGS1skeletal muscle — 1.9 nTPM, from PTGS1spleen — 7.0 nTPM, from PTGS1salivary gland — 3.6 nTPM, from PTGS1
0228 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 PTGS1 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

  • spinal cord4.1 nTPM
  • pituitary gland3.8 nTPM
  • midbrain2.8 nTPM
  • cerebral cortex2.7 nTPM
  • hippocampal formation2.5 nTPM
  • hypothalamus2.1 nTPM
  • amygdala1.4 nTPM
  • basal ganglia1.1 nTPM
  • retina0.7 nTPM
  • cerebellum0.3 nTPM

Peripheral and autonomic · 16

  • urinary bladder227.5 nTPM
  • colon102.0 nTPM
  • stomach 118.8 nTPM
  • small intestine17.4 nTPM
  • smooth muscle15.0 nTPM
  • heart muscle12.0 nTPM
  • lung10.6 nTPM
  • duodenum10.2 nTPM
  • kidney8.7 nTPM
  • spleen7.0 nTPM
  • salivary gland3.6 nTPM
  • liver2.8 nTPM
  • adrenal gland2.8 nTPM
  • thyroid gland2.7 nTPM
  • skeletal muscle1.9 nTPM
  • pancreas1.7 nTPM

Transcript is not protein. These are RNA levels for PTGS1, 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.

Equilibrium binding constants 7

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130

Functional readouts 28

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

TargetClassTypeValue (nM)pXOrganismAssay
Prostaglandin G/H synthase 1EnzymesIC504,0005.40Homo sapiensCHEMBL1008496
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291869
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291869
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291869
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291869
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291869
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291871
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291871
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291871
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291871
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909130
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291871
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
Prostaglandin G/H synthase 1EnzymesAC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL5291868
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