Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.1.20 extracted from

  • Rais, R.H.; Al Safarjalani, O.N.; Yadav, V.; Guarcello, V.; Kirk, M.; Chu, C.K.; Naguib, F.N.; el Kouni, M.H.
    6-Benzylthioinosine analogues as subversive substrate of Toxoplasma gondii adenosine kinase: activities and selective toxicities (2005), Biochem. Pharmacol., 69, 1409-1419.
    View publication on PubMed
Search for more literature for 2.7.1.20

Application

Application Comment Organism
medicine the enzyme is an excellent target for chemotherapy with 6-substituted purine nucleosides being potential selective antitoxoplasmic agents Toxoplasma gondii

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of the soluble enzyme in Escherichia coli strain BL21(DE3) Toxoplasma gondii

Inhibitors

Inhibitors Comment Organism Structure
2,4,6-trimethyl-6-benzylthioinosine
-
 Toxoplasma gondii
2,4-dichloro-6-benzylthioinosine
-
 Toxoplasma gondii
2-chloro-6-benzylthioinosine
-
 Toxoplasma gondii
2-chloro-6-fluoro-6-benzylthioinosine
-
 Toxoplasma gondii
2-fluoro-6-benzylthioinosine
-
 Toxoplasma gondii
2-methyl-6-benzylthioinosine
-
 Toxoplasma gondii
3,4-dichloro-6-benzylthioinosine
-
 Toxoplasma gondii
3-methyl-6-benzylthioinosine
-
 Toxoplasma gondii
3-nitro-6-benzylthioinosine
-
 Toxoplasma gondii
3-trifluoromethyl-6-benzylthioinosine
-
 Toxoplasma gondii
4-acetoxy-6-benzylthioinosine
-
 Toxoplasma gondii
4-bromo-6-benzylthioinosine
-
 Toxoplasma gondii
4-chloro-6-benzylthioinosine
-
 Toxoplasma gondii
4-cyano-6-benzylthioinosine
-
 Toxoplasma gondii
4-fluoro-6-benzylthioinosine
-
 Toxoplasma gondii
4-methoxy-6-benzylthioinosine
-
 Toxoplasma gondii
4-methyl-6-benzylthioinosine
-
 Toxoplasma gondii
4-nitro-6-benzylthioinosine
-
 Toxoplasma gondii
4-tert-butyl-6-benzylthioinosine
-
 Toxoplasma gondii
4-trifluoromethoxy-6-benzylthioinosine
-
 Toxoplasma gondii
6-benzylthioinosine
-
 Toxoplasma gondii
additional information IC50 values and toxicities, i.e. rates of survival, of the 6-benzylthioinosine derivatives in wild-type strain RH and in the mutant strain TgAK-3 in human fibrobalsts, effects of 6-benzylthioinosine and derivatives 2-cyano-6-benzylthioinosine and 2,4-dichloro-6-benzylthioinosine on survival of mice infected with the wild-type strain RH, overview Toxoplasma gondii
pyrimethamine
-
 Toxoplasma gondii
Sulfadiazine
-
 Toxoplasma gondii

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ at 5 mM MgCl2 Toxoplasma gondii

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
75000
-
 x * 75000, about, recombinant enzyme Toxoplasma gondii

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + adenosine Toxoplasma gondii enzyme shows highest activity of all enzymes involved in the adenosine salvage metabolism ADP + AMP
-
 ?

Organism

Organism UniProt Comment Textmining
Toxoplasma gondii
-
 wild-type strain RH and enzyme-deficient mutant strain TgAK-3, cultured in mice or human fibroblasts
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme from Escherichia coli strain BL21(DE3) by 3 steps of ion exchange chromatography, to homogeneity Toxoplasma gondii

Storage Stability

Storage Stability Organism
-75°C, pure enzyme, 20 mM Tris-HCl, pH 8.0, 15 mM 2-mercaptoethanol, stable for months Toxoplasma gondii

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + adenosine
-
 Toxoplasma gondii ADP + AMP
-
 ?
ATP + adenosine enzyme shows highest activity of all enzymes involved in the adenosine salvage metabolism Toxoplasma gondii ADP + AMP
-
 ?

Subunits

Subunits Comment Organism
? x * 75000, about, recombinant enzyme Toxoplasma gondii

Synonyms

Synonyms Comment Organism
AK
-
 Toxoplasma gondii

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Toxoplasma gondii

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Toxoplasma gondii

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0007
-
 2,4-dichloro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0009
-
 4-cyano-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0011
-
 4-nitro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0012
-
 4-fluoro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0013
-
 3-methyl-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0014
-
 2-chloro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0015
-
 2-methyl-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0021
-
 4-chloro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0024
-
 6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0025
-
 3,4-dichloro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0026
-
 4-methoxy-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0029
-
 3-trifluoromethyl-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.003
-
 3-nitro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0033
-
 4-methyl-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0075
-
 4-bromo-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.0377
-
 2-chloro-6-fluoro-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.096
-
 4-acetoxy-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.113
-
 4-tert-butyl-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.141
-
 4-trifluoromethoxy-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii
0.15
-
 2,4,6-trimethyl-6-benzylthioinosine pH 7.4, 37°C, recombinant enzyme Toxoplasma gondii