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Literature summary 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

Cloned(Commentary)

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

General Stability

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.25 1-phenyl-N-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]-1H-imidazole-5-carboxamide
-
 Entamoeba histolytica
2.7.1.25 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
2.7.1.25 2-(3-fluorophenoxy)-N-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]acetamide
-
 Entamoeba histolytica
2.7.1.25 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
2.7.1.25 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
2.7.1.25 3-(methanesulfonyl)-5,7-dimethyl[1,2]thiazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione
-
 Entamoeba histolytica
2.7.1.25 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
2.7.1.25 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
2.7.1.25 3-[7-(benzyloxy)-4,8-dimethyl-2-oxo-2H-1-benzopyran-3-yl]propanoic acid
-
 Entamoeba histolytica
2.7.1.25 4-(3-methoxyphenyl)-5-(phenylmethanesulfonyl)-1H-tetrazol-4-ium
-
 Entamoeba histolytica
2.7.1.25 5-bromo-2-chloro-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)benzamide
-
 Entamoeba histolytica
2.7.1.25 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
2.7.1.25 auranofin shows good docking results. The inhibitor halts not only Entamoeba trophozoite proliferation but also cyst formation Entamoeba histolytica
2.7.1.25 delamanid
-
 Entamoeba histolytica
2.7.1.25 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
2.7.1.25 N,N'-[furan-2,5-diylbis(2-chloro-4,1-phenylene)]diguanidine
-
 Entamoeba histolytica
2.7.1.25 N,N'-[furan-2,5-diylbis(3-chloro-4,1-phenylene)]diguanidine
-
 Entamoeba histolytica
2.7.1.25 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)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.25 Entamoeba histolytica C4LUW9
-
-

Purification (Commentary)

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.25 trophozoite
-
 Entamoeba histolytica
-

Storage Stability

EC Number Storage Stability Organism
2.7.1.25 -30°C, rEhAPSK activity is almost entirely absent after storage for 3 days or more, due to precipitation Entamoeba histolytica
2.7.1.25 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)

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

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.1.25 37
-
 assay at Entamoeba histolytica

Temperature Stability [°C]

EC Number Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
2.7.1.25 95
-
 purified recombinant enzyme, 10 min, inactivation and denaturation Entamoeba histolytica

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.1.25 8
-
 assay at Entamoeba histolytica

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.25 0.00047
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica N,N'-[furan-2,5-diylbis(2-chloro-4,1-phenylene)]diguanidine
2.7.1.25 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
2.7.1.25 0.00138
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica auranofin
2.7.1.25 0.00203
-
 pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica N,N'-[furan-2,5-diylbis(3-chloro-4,1-phenylene)]diguanidine
2.7.1.25 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
2.7.1.25 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
2.7.1.25 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
2.7.1.25 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
2.7.1.25 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
2.7.1.25 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
2.7.1.25 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
2.7.1.25 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
2.7.1.25 0.01
-
 above, pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica 4-(3-methoxyphenyl)-5-(phenylmethanesulfonyl)-1H-tetrazol-4-ium
2.7.1.25 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
2.7.1.25 0.01
-
 above, pH 8.0, 37°C, recombinant enzyme Entamoeba histolytica delamanid

General Information

EC Number General Information Comment Organism
2.7.1.25 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