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Literature summary for 2.7.1.25 extracted from

  • Mi-Ichi, F.; Ishikawa, T.; Tam, V.K.; Deloer, S.; Hamano, S.; Hamada, T.; Yoshida, H.
    Characterization of Entamoeba histolytica adenosine 5-phosphosulfate (APS) kinase, validation as a target and provision of leads for the development of new drugs against amoebiasis (2019), PLoS Negl. Trop. Dis., 13, e0007633 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.25

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of His-tagged enzyme in Escherichia coli strain BL21(DE3) Entamoeba histolytica

General Stability

General Stability Organism
recombinant EhAPSK activity is labile to freeze-thaw because of aggregation Entamoeba histolytica

Inhibitors

Inhibitors Comment Organism Structure
1-phenyl-N-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]-1H-imidazole-5-carboxamide
-
 Entamoeba histolytica
2-(3-fluorophenoxy)-N-[4-(2-pyridyl)thiazol-2-yl]acetamide shows good docking results. The inhibitor halts not only Entamoeba trophozoite proliferation but also cyst formation Entamoeba histolytica
2-(3-fluorophenoxy)-N-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]acetamide
-
 Entamoeba histolytica
2-cycloheptyl-4-(4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
 Entamoeba histolytica
2-cycloheptyl-5-(4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one
-
 Entamoeba histolytica
3-(methanesulfonyl)-5,7-dimethyl[1,2]thiazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione
-
 Entamoeba histolytica
3-phenyl-N-[4-(2-pyridyl)thiazol-2-yl]imidazole-4-carboxamide shows good docking results. The inhibitor halts not only Entamoeba trophozoite proliferation but also cyst formation Entamoeba histolytica
3-[5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-N-[(1-hydroxy-3,3-dimethyl-1,3-dihydro-2,1-benzoxaborol-5-yl)methyl]-5-methylbenzamide
-
 Entamoeba histolytica
3-[7-(benzyloxy)-4,8-dimethyl-2-oxo-2H-1-benzopyran-3-yl]propanoic acid
-
 Entamoeba histolytica
4-(3-methoxyphenyl)-5-(phenylmethanesulfonyl)-1H-tetrazol-4-ium
-
 Entamoeba histolytica
5-bromo-2-chloro-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)benzamide
-
 Entamoeba histolytica
8-(4-methyl-3-[3-[([2-methyl-5-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl)amino]benzamido]benzamido)naphthalene-1,3,5-trisulfonic acid
-
 Entamoeba histolytica
auranofin shows good docking results. The inhibitor halts not only Entamoeba trophozoite proliferation but also cyst formation Entamoeba histolytica
delamanid
-
 Entamoeba histolytica
additional information validation of in silico molecular docking analysis and an in vitro enzyme activity assay for large scale screening. Inhibitor screening, In silico molecular docking analysis and simulation ranks the binding free energy between a homology modeling structure of EhAPSK and 400 compounds, overview. Analysis of the cytotoxicity Entamoeba histolytica
N,N'-[furan-2,5-diylbis(2-chloro-4,1-phenylene)]diguanidine
-
 Entamoeba histolytica
N,N'-[furan-2,5-diylbis(3-chloro-4,1-phenylene)]diguanidine
-
 Entamoeba histolytica
N-[2-(5-chloro-2-methoxyanilino)-2-oxoethyl]-N-methyl-2-phenyl-2H-1,2,3-triazole-4-carboxamide
-
 Entamoeba histolytica

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + adenylyl sulfate Entamoeba histolytica
-
 ADP + 3'-phosphoadenylyl sulfate
-
 ?

Organism

Organism UniProt Comment Textmining
Entamoeba histolytica C4LUW9
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Entamoeba histolytica

Source Tissue

Source Tissue Comment Organism Textmining
trophozoite
-
 Entamoeba histolytica
-

Storage Stability

Storage Stability Organism
-30°C, rEhAPSK activity is almost entirely absent after storage for 3 days or more, due to precipitation Entamoeba histolytica
4°C, the specific activity of rEhAPSK after storage for 3 months is about 25% relative to that of freshly purified samples, due to precipitation Entamoeba histolytica

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + adenylyl sulfate
-
 Entamoeba histolytica ADP + 3'-phosphoadenylyl sulfate
-
 ?

Synonyms

Synonyms Comment Organism
adenosine 5'-phosphosulfate kinase
-
 Entamoeba histolytica
EhAPSK
-
 Entamoeba histolytica
EHI_179080
-
 Entamoeba histolytica

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Entamoeba histolytica

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
95
-
 purified recombinant enzyme, 10 min, inactivation and denaturation Entamoeba histolytica

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Entamoeba histolytica

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00047
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica N,N'-[furan-2,5-diylbis(2-chloro-4,1-phenylene)]diguanidine
0.00052
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 8-(4-methyl-3-[3-[([2-methyl-5-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl)amino]benzamido]benzamido)naphthalene-1,3,5-trisulfonic acid
0.00138
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica auranofin
0.00203
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica N,N'-[furan-2,5-diylbis(3-chloro-4,1-phenylene)]diguanidine
0.00427
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 2-cycloheptyl-4-(4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
0.00473
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 2-cycloheptyl-5-(4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one
0.00573
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 3-[5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-N-[(1-hydroxy-3,3-dimethyl-1,3-dihydro-2,1-benzoxaborol-5-yl)methyl]-5-methylbenzamide
0.0063
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 2-(3-fluorophenoxy)-N-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]acetamide
0.00657
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica N-[2-(5-chloro-2-methoxyanilino)-2-oxoethyl]-N-methyl-2-phenyl-2H-1,2,3-triazole-4-carboxamide
0.00675
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 1-phenyl-N-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]-1H-imidazole-5-carboxamide
0.00767
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 3-[7-(benzyloxy)-4,8-dimethyl-2-oxo-2H-1-benzopyran-3-yl]propanoic acid
0.00867
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 3-(methanesulfonyl)-5,7-dimethyl[1,2]thiazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione
0.01
-
 above, pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 4-(3-methoxyphenyl)-5-(phenylmethanesulfonyl)-1H-tetrazol-4-ium
0.01
-
 above, pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 5-bromo-2-chloro-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)benzamide
0.01
-
 above, pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica delamanid

General Information

General Information Comment Organism
additional information homology modeling of the APSK domain structure of EhAPSK using three structures as templates (PDB IDs: 3UIE, 4FXP, and 2GKS), overview. All combinations of the three predicted structures are calculated by visual molecular dynamics Entamoeba histolytica