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Prostaglandin synthases C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Subsequent to the formation of PGH2, the cytochrome P450 activities thromboxane synthase (CYP5A1, TBXAS1, P24557 , EC 5.3.99.5) and prostacyclin synthase (CYP8A1, PTGIS, Q16647, EC 5.3.99.4) generate thromboxane A2 and prostacyclin (PGI2), respectively. Additionally, multiple enzyme activities are able to generate prostaglandin E2 (PGE2), prostaglandin D2 (PGD2) and prostaglandin F (PGF). PGD2 can be metabolised to 9α,11β-prostacyclin F through the multifunctional enzyme activity of AKR1C3. PGE2 can be metabolised to 9α,11β-prostaglandin F through the 9-ketoreductase activity of CBR1. Conversion of the 15-hydroxyecosanoids, including prostaglandins, lipoxins and leukotrienes to their keto derivatives by the NAD-dependent enzyme HPGD leads to a reduction in their biological activity.

Enzymes

1378
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Thromboxane-A synthase (CYP5A1) C Show summary » More detailed page go icon to follow link

Prostacyclin synthase (CYP8A1) C Show summary »

mPGES1 C Show summary » More detailed page go icon to follow link

mPGES2 C Show summary »


Target Id 1378
Nomenclature mPGES2
Previous and unofficial names microsomal prostaglandin E synthase 2 | mPGES-2 | GBF1 | GBF-1
Genes PTGES2 (Hs), Ptges2 (Mm), Ptges2 (Rn)
Ensembl ID ENSG00000148334 (Hs), ENSMUSG00000026820 (Mm), ENSRNOG00000014050 (Rn)
UniProtKB AC Q9H7Z7 (Hs), Q8BWM0 (Mm)
EC number
5.3.99.3 PGH2 = PGE2
Cofactors
dihydrolipoic acid [27]
Inhibitors
compound 30 [PMID: 15953724] pIC50 <6.0 [23]
Comment Heme-free mPGES2 catalyses the isomerisation of prostaglandin H2 (PGE2) to prostaglandin E2 (PGE2) in the presence of glutathione (GSH); in contrast heme-bound mPGES2 catalyses the degradation of PGH2 to 12-hydroxyheptadecatrienoic acid (HHT) and malondialdehyde (MDA) [26,29-30]. In colon cancer cells artemisinin has been reported to bind reversibly to mPGES2 (occupying the PGH2 site), with the effect of blocking PGE2 biosynthesis and inhibiting cell proliferation [4].

cPGES C Show summary »

L-PGDS C Show summary »

H-PGDS C Show summary »

AKR1C3 C Show summary » More detailed page go icon to follow link

CBR1 C Show summary »

HPGD C Show summary » More detailed page go icon to follow link

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.