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Literature summary for 1.14.99.1 extracted from

  • Ramkissoon, A.; Wells, P.G.
    Human prostaglandin H synthase (hPHS)-1 and hPHS-2 in amphetamine analog bioactivation, DNA oxidation, and cytotoxicity (2011), Toxicol. Sci., 120, 154-162.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
arachidonate
-
Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
stable expression of PHS-1 and PHS-2 in CHO-K1 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Acetylsalicylic acid an irreversible inhibitor of both hPHS-1 and hPHS-2 Homo sapiens
DUP-697 a PHS-2-specific inhibitor Homo sapiens
SC-560 a PHS-1-specific inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
arachidonate + AH2 + O2 Homo sapiens
-
prostaglandin H2 + A + H2O
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + AH2 + O2
-
Homo sapiens prostaglandin H2 + A + H2O
-
?

Synonyms

Synonyms Comment Organism
PHS-1
-
Homo sapiens
PHS-2
-
Homo sapiens
prostaglandin H synthase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

General Information

General Information Comment Organism
additional information neurotoxicity of the amphetamine analogues methamphetamine and 3,4-methylenedioxyamphetamine, the active metabolite of ecstasy, may involve their prostaglandin H synthase-dependent bioactivation to free radical intermediates that generate reactive oxygen species and oxidatively damage cellular macromolecules. The activation effect is blocked by irreversible enzyme inhibitor acetylsalicylic acid, overview Homo sapiens