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Literature summary for 3.5.4.3 extracted from

  • Ujjinamatada, R.K.; Bhan, A.; Hosmane, R.S.
    Design of inhibitors against guanase: Synthesis and biochemical evaluation of analogues of azepinomycin (2006), Bioorg. Med. Chem. Lett., 16, 5551-5554.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-benzyl-6-(hydroxymethyl)-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione competitive; competitive, the presence of a benzyl group at position-3 enhances the inhibitory activity by greater than twofold as compared to that without the benzyl group Oryctolagus cuniculus
6-(hydroxymethyl)-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione competitive; competitive, the presence of a benzyl group at position-3 enhances the inhibitory activity by greater than twofold as compared to that without the benzyl group Oryctolagus cuniculus
6-hydroxy-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione i.e. azepinomycin Oryctolagus cuniculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics Oryctolagus cuniculus
0.00966
-
guanine pH 7.4, 25°C Oryctolagus cuniculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
guanine + H2O Oryctolagus cuniculus
-
xanthine + NH3
-
?

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus
-
-
-
Oryctolagus cuniculus
-
commercial preparation
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation from liver Oryctolagus cuniculus
-
liver
-
Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
guanine + H2O
-
Oryctolagus cuniculus xanthine + NH3
-
?
guanine + H2O reaction via tetrahedral intermediate Oryctolagus cuniculus xanthine + NH3
-
?

Synonyms

Synonyms Comment Organism
GDA
-
Oryctolagus cuniculus
guanase
-
Oryctolagus cuniculus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Oryctolagus cuniculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Oryctolagus cuniculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0005
-
6-hydroxy-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione pH 7.4, 25°C Oryctolagus cuniculus
0.00201
-
3-benzyl-6-(hydroxymethyl)-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione pH 7.4, 25°C Oryctolagus cuniculus
0.00536
-
6-(hydroxymethyl)-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione pH 7.4, 25°C Oryctolagus cuniculus
0.02
-
3-benzyl-6-(hydroxymethyl)-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione pH 7.4, 25°C Oryctolagus cuniculus
0.054
-
6-(hydroxymethyl)-3,4,6,7-tetrahydroimidazo[4,5-e][1,4]diazepine-5,8-dione pH 7.4, 25°C Oryctolagus cuniculus