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Literature summary for 2.3.1.30 extracted from

  • Agarwal, S.; Jain, R.; Bhattacharya, A.; Azam, A.
    Inhibitors of Escherichia coli serine acetyltransferase block proliferation of Entamoeba histolytica trophozoites (2008), Int. J. Parasitol., 38, 137-141.
    View publication on PubMed
Search for more literature for 2.3.1.30

Application

Application Comment Organism
medicine inhibition of enzyme blocks growth of parasite trophozoites but not of mouse cell culture Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
2-amino-9-(naphthalen-2-yl)-9H-purin-6-ol 0.05 microg/microl showing 38% inhibition in the presence of 0.10 mM acetyl-CoA, binding to active site Escherichia coli
2-amino-9-naphthalen-2-yl-9H-purin-6-ol
-
 Entamoeba histolytica
3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[3,4-d]thieno[2,3-b]pyridine-7-carboxylate most potent inhibitor, 0.05 microg/microl showing 50% inhibition in the presence of 0.10 mM acetyl-CoA, binding to active site, increasing Km, decreasing Vmax Escherichia coli
3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[3,4-d]thieno[2,3-b]pyridine-7-carboxylic acid
-
 Entamoeba histolytica
4,10-dihydroxy-1,7-phenanthroline-3,9-dicarboxylate 0.05 microg/microl showing 24% inhibition in the presence of 0.10 mM acetyl-CoA, binding to active site Escherichia coli
4,10-dihydroxy-1,7-phenanthroline-3,9-dicarboxylic acid
-
 Entamoeba histolytica
additional information no growth inhibition of mouse cell culture with 4,10-dihydroxy-1,7-phenanthroline-3,9-dicarboxylic acid, 2-amino-9-naphthalen-2-yl-9H-purin-6-ol, or 3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[3,4-d]thieno[2,3-b]pyridine-7-carboxylic acid in a MTT assay Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-serine + acetyl-CoA Mus musculus
-
 O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA Escherichia coli
-
 O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA Entamoeba histolytica
-
 O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA Escherichia coli DH5-alpha
-
 O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA Entamoeba histolytica HMM1:IMSS
-
 O-acetyl-L-serine + CoA
-
 ?

Organism

Organism UniProt Comment Textmining
Entamoeba histolytica Q9U8X2 trophozoite
-
Entamoeba histolytica HMM1:IMSS Q9U8X2 trophozoite
-
Escherichia coli P0A9D4
-
-
Escherichia coli DH5-alpha P0A9D4
-
-
Mus musculus
-
 mouse cell line
-

Purification (Commentary)

Purification (Comment) Organism
cells centrifuged, resuspended in 0.01 M Tris-HCl, pH 7.5, sonicated, centrifuged, supernatant subjected to streptomycin sulfate (10%) and ammonium sulfate (70%) precipitation, precipitated protein dissolved in same buffer, desalted on a G-25 column Mus musculus
cells centrifuged, resuspended in 0.01 M Tris-HCl, pH 7.5, sonicated, centrifuged, supernatant subjected to streptomycin sulfate (10%) and ammonium sulfate (70%) precipitation, precipitated protein dissolved in same buffer, desalted on a G-25 column Escherichia coli

Source Tissue

Source Tissue Comment Organism Textmining
Vero cell C-1008 cell line Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-serine + acetyl-CoA
-
 Mus musculus O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA
-
 Escherichia coli O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA
-
 Entamoeba histolytica O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA
-
 Escherichia coli DH5-alpha O-acetyl-L-serine + CoA
-
 ?
L-serine + acetyl-CoA
-
 Entamoeba histolytica HMM1:IMSS O-acetyl-L-serine + CoA
-
 ?

Subunits

Subunits Comment Organism
trimer 3 * x, predicted from homology modeling with Escherichia coli enzyme crystal structure Entamoeba histolytica

Synonyms

Synonyms Comment Organism
SATase
-
 Mus musculus
SATase
-
 Escherichia coli
SATase
-
 Entamoeba histolytica
serine acetyltransferase
-
 Mus musculus
serine acetyltransferase
-
 Escherichia coli
serine acetyltransferase
-
 Entamoeba histolytica

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.042
-
 3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[3,4-d]thieno[2,3-b]pyridine-7-carboxylic acid 72 micromol, 0.1 M Tris-HCl, pH 7.5, room temperature Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00061
-
 count of viable trophozoites after 72 h compared to control measured with 32.16, 64.32, and 160.8 microM inhibitor Entamoeba histolytica 3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[3,4-d]thieno[2,3-b]pyridine-7-carboxylic acid
0.00107
-
 count of viable trophozoites after 72 h compared to control measured with 32.16, 64.32, and 160.8 microM inhibitor Entamoeba histolytica 4,10-dihydroxy-1,7-phenanthroline-3,9-dicarboxylic acid
0.00152
-
 count of viable trophozoites after 72 h compared to control measured with 32.16, 64.32, and 160.8 microM inhibitor Entamoeba histolytica 2-amino-9-naphthalen-2-yl-9H-purin-6-ol
0.072
-
 72 micromol, 0.1 M Tris-HCl, pH 7.5, room temperature Escherichia coli 3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[3,4-d]thieno[2,3-b]pyridine-7-carboxylic acid

General Information

General Information Comment Organism
malfunction compounds that (partially) block the Escherichia coli enzyme activity block the growth of Entamoeba histolytica trophozoites but not mammalian cells Mus musculus
malfunction compounds that (partially) block the Escherichia coli enzyme activity block the growth of Entamoeba histolytica trophozoites but not mammalian cells Escherichia coli
malfunction compounds that (partially) block the Escherichia coli enzyme activity block the growth of Entamoeba histolytica trophozoites but not mammalian cells Entamoeba histolytica