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Literature summary extracted from

  • Poinas, A.; Backers, K.; Riley, A.M.; Mills, S.J.; Moreau, C.; Potter, B.V.; Erneux, C.
    Interaction of the catalytic domain of inositol 1,4,5-trisphosphate 3-kinase A with inositol phosphate analogues (2005), Chembiochem, 6, 1449-1457.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.127 stable expression of the C-terminal catalytic domain 3KA-cat30, comprising residues Ser185-Arg459, as N-terminally His-tagged and S-tagged protein in Escherichia coli strain BL21(DE3) Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.127 (2'S)-1D-1,2-O-[(2'-phosphoryloxy)propane-1',3'-diyl]-myo-inositol 4,5-bisphosphate synthetic bicyclic inositol trisphosphate S epimer, IC50 is 0.156 mM Rattus norvegicus
2.7.1.127 1D-myo-inositol 1,3,4,5-tetrakisphosphate product inhibition, IC50 is 0.013 mM Rattus norvegicus
2.7.1.127 D-2-deoxyinositol 1,3,4,5-tetrakisphosphate strong inhibition of isozyme A, IC50 is 0.0054 mM Rattus norvegicus
2.7.1.127 D-2-deoxyinositol 1,4,5-trisphosphate strong inhibition of isozyme A, IC50 is 0.0017 mM Rattus norvegicus
2.7.1.127 D-3-deoxyinositol 1,4,6-trisphosphate strong inhibition of isozyme A, IC50 is 0.0014 mM Rattus norvegicus
2.7.1.127 D-6-deoxyinositol 1,3,4,5-tetrakisphosphate strong inhibition of isozyme A, IC50 is 0.0051 mM Rattus norvegicus
2.7.1.127 D-myo-inositol 2,4,5-trisphosphate IC50 is 0.117 mM Rattus norvegicus
2.7.1.127 additional information poor inhibition by adenophostin analogues xylo-furanophostin and furanophostin, by L-myo-inositol 2,4,5-trisphosphate, synthetic bicyclic inositol trisphosphate R epimer, and by epi-1D-myo-inositol 1,3,6-trisphosphate Rattus norvegicus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.1.127 Mg2+
-
 Rattus norvegicus
2.7.1.127 additional information assay in presence of Triton X-100 and ethylene glycol bis-(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.127 ATP + 1D-myo-inositol 1,4,5-trisphosphate Rattus norvegicus
-
 ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.127 Rattus norvegicus
-
 isozyme A
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.127 recombinant N-terminally His-tagged and S-tagged C-terminal catalytic domain 3KA-cat30, comprising residues Ser185-Arg459, from Escherichia coli strain BL21(DE3) by nickel and S-protein affinity chromatography, and gel filtration Rattus norvegicus

Reaction

EC Number Reaction Comment Organism Reaction ID
2.7.1.127 ATP + 1D-myo-inositol 1,4,5-trisphosphate = ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate catalytic mechanism involving the 3-hydroxygroup of the substrate, substrate recognition Rattus norvegicus
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.127 ATP + 1D-myo-inositol 1,4,5-trisphosphate
-
 Rattus norvegicus ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate
-
 ?
2.7.1.127 ATP + D-2-deoxy-myo-inositol 1,4,5-trisphosphate
-
 Rattus norvegicus ADP + D-2-deoxy-myo-inositol 1,3,4,5-tetrakisphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.127 inositol 1,4,5-trisphosphate 3-kinase A
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.1.127 37
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.1.127 7.5
-
 assay at Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.127 ATP
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.127 0.0014
-
 strong inhibition of isozyme A, IC50 is 0.0014 mM Rattus norvegicus D-3-deoxyinositol 1,4,6-trisphosphate
2.7.1.127 0.0017
-
 strong inhibition of isozyme A, IC50 is 0.0017 mM Rattus norvegicus D-2-deoxyinositol 1,4,5-trisphosphate
2.7.1.127 0.0051
-
 strong inhibition of isozyme A, IC50 is 0.0051 mM Rattus norvegicus D-6-deoxyinositol 1,3,4,5-tetrakisphosphate
2.7.1.127 0.0054
-
 strong inhibition of isozyme A, IC50 is 0.0054 mM Rattus norvegicus D-2-deoxyinositol 1,3,4,5-tetrakisphosphate
2.7.1.127 0.013
-
 product inhibition, IC50 is 0.013 mM Rattus norvegicus 1D-myo-inositol 1,3,4,5-tetrakisphosphate
2.7.1.127 0.117
-
 IC50 is 0.117 mM Rattus norvegicus D-myo-inositol 2,4,5-trisphosphate
2.7.1.127 0.156
-
 synthetic bicyclic inositol trisphosphate S epimer, IC50 is 0.156 mM Rattus norvegicus (2'S)-1D-1,2-O-[(2'-phosphoryloxy)propane-1',3'-diyl]-myo-inositol 4,5-bisphosphate