Literature summary for 2.7.1.127 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.

Search for more literature for 2.7.1.127

Cloned(Commentary)

Cloned (Comment)	Organism
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

Inhibitors	Comment	Organism	Structure
(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
1D-myo-inositol 1,3,4,5-tetrakisphosphate	product inhibition, IC50 is 0.013 mM	Rattus norvegicus
D-2-deoxyinositol 1,3,4,5-tetrakisphosphate	strong inhibition of isozyme A, IC50 is 0.0054 mM	Rattus norvegicus
D-2-deoxyinositol 1,4,5-trisphosphate	strong inhibition of isozyme A, IC50 is 0.0017 mM	Rattus norvegicus
D-3-deoxyinositol 1,4,6-trisphosphate	strong inhibition of isozyme A, IC50 is 0.0014 mM	Rattus norvegicus
D-6-deoxyinositol 1,3,4,5-tetrakisphosphate	strong inhibition of isozyme A, IC50 is 0.0051 mM	Rattus norvegicus
D-myo-inositol 2,4,5-trisphosphate	IC50 is 0.117 mM	Rattus norvegicus
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

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Rattus norvegicus
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)

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

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	isozyme A	-

Purification (Commentary)

Purification (Comment)	Organism
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

Reaction	Comment	Organism	Reaction ID
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)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Rattus norvegicus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0014	-	strong inhibition of isozyme A, IC50 is 0.0014 mM	Rattus norvegicus	D-3-deoxyinositol 1,4,6-trisphosphate
0.0017	-	strong inhibition of isozyme A, IC50 is 0.0017 mM	Rattus norvegicus	D-2-deoxyinositol 1,4,5-trisphosphate
0.0051	-	strong inhibition of isozyme A, IC50 is 0.0051 mM	Rattus norvegicus	D-6-deoxyinositol 1,3,4,5-tetrakisphosphate
0.0054	-	strong inhibition of isozyme A, IC50 is 0.0054 mM	Rattus norvegicus	D-2-deoxyinositol 1,3,4,5-tetrakisphosphate
0.013	-	product inhibition, IC50 is 0.013 mM	Rattus norvegicus	1D-myo-inositol 1,3,4,5-tetrakisphosphate
0.117	-	IC50 is 0.117 mM	Rattus norvegicus	D-myo-inositol 2,4,5-trisphosphate
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

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Release 2023.1 (January 2023)