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Literature summary for 3.5.4.4 extracted from

  • Kuno, M.; Seki, N.; Tsujimoto, S.; Nakanishi, I.; Kinoshita, T.; Nakamura, K.; Terasaka, T.; Nishio, N.; Sato, A.; Fujii, T.
    Anti-inflammatory activity of non-nucleoside adenosine deaminase inhibitor FR234938 (2006), Eur. J. Pharmacol., 534, 241-249.
    View publication on PubMed

Application

Application Comment Organism
drug development enzyme inhibitor FR234938 might be effective as an anti-rheumatic and anti-inflammatory drug by modulating the host-defense concentrations of adenosine Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
enzyme expression in an enzyme-deficient Escherichia coli strain Sphi3834 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
FR234938 i.e. 1-((1R,2S)-2-hydroxy-1-(2-(1-naphthyl)ethyl)propyl)1H-imidazole-4-carboxamine, a non-nucleoside inhibitor, the inhibition is blocked by an A2a adenosine receptor antagonist Homo sapiens
pentostatin i.e. (8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydro-2-furanyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2'-deoxyadenosine + H2O Homo sapiens
-
2'-deoxyinosine + NH3
-
ir
adenosine + H2O Homo sapiens metabolization of extracellular adenosine leads to exacerbation of inflammation inosine + NH3
-
ir

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
SKW6.4 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2'-deoxyadenosine + H2O
-
Homo sapiens 2'-deoxyinosine + NH3
-
ir
adenosine + H2O metabolization of extracellular adenosine leads to exacerbation of inflammation Homo sapiens inosine + NH3
-
ir
adenosine + H2O metabolization of extracellular adenosine Homo sapiens inosine + NH3
-
ir

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000027
-
pH 7.4, 22°C Homo sapiens FR234938