Activating Compound | Comment | Organism | Structure |
---|---|---|---|
2,5-O-benzyl-myo-inositol 1,3,4,6-tetrakisphosphate | activates the ATP hydrolysis activity and inhibits the InsP6 kinase activity of the enzyme | Homo sapiens | |
2-O-aminoethyl-myo-inositol 1,2,3,4,6-pentakisphosphate | - |
Homo sapiens | |
2-O-benzoyl-myo-inositol 1,2,3,4,6-pentakisphosphate | - |
Homo sapiens | |
2-O-benzyl-5-O-alpha-phosphonoacetyl-myo-inositol 1,3,4,6-tetrakisphosphate | stimulates ATP hydrolysis 9fold | Homo sapiens | |
2-O-benzyl-5-O-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate | - |
Homo sapiens | |
2-O-benzyl-myo-inositol 1,2,3,4,6-pentakisphosphate | - |
Homo sapiens | |
2-O-butanoyl-myo-inositol 1,2,3,4,6-pentakisphosphate | - |
Homo sapiens | |
5-O-alpha-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate | - |
Homo sapiens | |
5-O-alpha-phoshonoacetyl-myo-inositol 1,3,4,6-tetrakisphosphate | - |
Homo sapiens | |
5-O-alpha-phosphonoacetyl-myo-inositol 1,2,3,4,6-pentakisphosphate | stimulates ATP hydrolysis 5fold | Homo sapiens | |
additional information | synthesis and effects of inositol phosphates and analogues upon ATPase activity, overview. The compounds are also inhibitors of [PP]2-InsP4 dephosphorylation. Binding structures, overview | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
recombinant expression of wild-type and mutant enzymes | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
N-terminally truncated PPIP5K2 kinase mutant, residues 41-366, hanging drop vapor diffusion against a well buffer of 12% w/v PEG 3350, 20 mM MgCl2, 0.1 M HEPES, pH 7.0, 0,1 mM AMP-PNP, and 2 mM CdCl2 at 4°C, 3 days, 4°C, X-ray diffraction structure determination and analysis | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
E192G | site-directed mutagenesis | Homo sapiens |
E192Q | site-directed mutagenesis | Homo sapiens |
K103A | site-directed mutagenesis | Homo sapiens |
K213A | site-directed mutagenesis | Homo sapiens |
K54A | site-directed mutagenesis | Homo sapiens |
additional information | construction of an N-terminally truncated mutant PPIP5K2KD comprising residues 41-366 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,5-O-benzyl-myo-inositol 1,3,4,6-tetrakisphosphate | activates the ATP hydrolysis activity and inhibits the PPIP5K2 activity and InsP6 kinase activity, and the 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme. The compound can inhibit inositol phosphate kinase activity without occupying the catalytic site | Homo sapiens | |
2-O-benzyl-5-O-alpha-phosphonoacetyl-myo-inositol 1,3,4,6-tetrakisphosphate | stimulates ATP hydrolysis 9fold, but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme. The compound can inhibit inositol phosphate kinase activity without occupying the catalytic site | Homo sapiens | |
2-O-benzyl-5-O-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate | activates ATP hydrolysis activity but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme | Homo sapiens | |
2-O-benzyl-myo-inositol 1,2,3,4,6-pentakisphosphate | activates ATP hydrolysis activity but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme | Homo sapiens | |
5-O-alpha-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate | activates ATP hydrolysis activity but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme | Homo sapiens | |
5-O-alpha-phosphonoacetyl-myo-inositol 1,2,3,4,6-pentakisphosphate | stimulates ATP hydrolysis 5fold, but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme | Homo sapiens | |
additional information | synthesis and effects of inositol phosphates and analogues upon ATPase activity, overview. The compounds are also inhibitors of [PP]2-InsP4 dephosphorylation. Binding structures, overview | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 1D-myo-inositol 5-diphosphate 1,2,3,4,6-pentakisphosphate | Homo sapiens | - |
ADP + 1D-myo-inositol 1,5-bis(diphosphate) 2,3,4,6-tetrakisphosphate | - |
? | |
ATP + 1D-myo-inositol hexakisphosphate | Homo sapiens | - |
ADP + 1D-myo-inositol 1-diphosphate 2,3,4,5,6-pentakisphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O43314 | isozyme PPIP5K2 | - |
Purification (Comment) | Organism |
---|---|
recombinant wild-type and truncated mutant enzymes | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 1D-myo-inositol 5-diphosphate 1,2,3,4,6-pentakisphosphate | - |
Homo sapiens | ADP + 1D-myo-inositol 1,5-bis(diphosphate) 2,3,4,6-tetrakisphosphate | - |
? | |
ATP + 1D-myo-inositol hexakisphosphate | - |
Homo sapiens | ADP + 1D-myo-inositol 1-diphosphate 2,3,4,5,6-pentakisphosphate | - |
? | |
additional information | the bifunctional enzyme also catalyzes the reaction of EC 2.7.4.21, InsP6 kinase. The enzyme exhibits an unusual, nonproductive, substrate-stimulated ATPase activity, that is stimulated by the natural substrates and by 5-O-alpha-phosphonoacetyl-myo-inositol 1,2,3,4,6-pentakisphosphate and 2-O-benzyl-5-O-alpha-phosphonoacetyl-myo-inositol 1,3,4,6-tetrakisphosphate. It also shows 1,5-[PP]2-InsP4 dephosphorylation activity. The enzyme has two adjacent ligand-binding sites, the architecture of this second ligand-binding site is represented by a deep cleft, which is walled on one side by K53, K54, and K103. The opposite face is formed from R213, and a loop created from residues E192 to H194 | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
diphosphoinositol pentakisphosphate kinase 2 | - |
Homo sapiens |
More | cf. EC 2.7.4.21 | Homo sapiens |
PPIP5K2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | 7.5 | assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00014 | - |
inhibition of the 1,5-[PP]2-InsP4 dephosphorylation, pH 7.0, 37°C | Homo sapiens | 5-O-alpha-phosphonoacetyl-myo-inositol 1,2,3,4,6-pentakisphosphate | |
0.00017 | - |
inhibition of the 1,5-[PP]2-InsP4 dephosphorylation, pH 7.0, 37°C | Homo sapiens | 2,5-O-benzyl-myo-inositol 1,3,4,6-tetrakisphosphate | |
0.00042 | - |
inhibition of the 1,5-[PP]2-InsP4 dephosphorylation, pH 7.0, 37°C | Homo sapiens | 2-O-benzyl-5-O-alpha-phosphonoacetyl-myo-inositol 1,3,4,6-tetrakisphosphate | |
0.00044 | - |
inhibition of the 1,5-[PP]2-InsP4 dephosphorylation, pH 7.0, 37°C | Homo sapiens | 2-O-benzyl-myo-inositol 1,2,3,4,6-pentakisphosphate | |
0.0005 | - |
inhibition of the 1,5-[PP]2-InsP4 dephosphorylation, pH 7.0, 37°C | Homo sapiens | 2-O-benzyl-5-O-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate | |
0.0024 | - |
inhibition of the 1,5-[PP]2-InsP4 dephosphorylation, pH 7.0, 37°C | Homo sapiens | 5-O-alpha-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate |