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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).
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 F2α (PGF2α). PGD2 can be metabolised to 9α,11β-prostacyclin F2α through the multifunctional enzyme activity of AKR1C3. PGE2 can be metabolised to 9α,11β-prostaglandin F2α 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.
Thromboxane-A synthase (CYP5A1) C Show summary » More detailed page |
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Prostacyclin synthase (CYP8A1) C Show summary » |
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mPGES1 C Show summary » More detailed page |
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mPGES2 C Show summary »
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cPGES C Show summary » |
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L-PGDS C Show summary » |
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H-PGDS C Show summary » |
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AKR1C3 C Show summary » More detailed page |
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CBR1 C Show summary » |
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HPGD C Show summary » More detailed 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.
YS121 has been reported to inhibit mPGES1 and 5-LOX with a pIC50 value of 5.5 [16].