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Literature summary for 2.7.1.153 extracted from

  • Dickson, J.; Lee, W.; Shepherd, P.; Buchanan, C.
    Enzyme activity effects of N-terminal His-tag attached to catalytic sub-unit of phosphoinositide-3-kinase (2013), Biosci. Rep., 33, 857-863.
No PubMed abstract available

Cloned(Commentary)

Cloned (Comment) Organism
recombinant coexpression of N-terminally His-tagged full-length wild-type and mutant class 1a isoform catalytic subunits with the p85 regulatory subunit, impacct of the His-tag on the catalytic activity, overview Homo sapiens
recombinant coexpression of N-terminally His-tagged full-length wild-type and mutant class 1b isoform catalytic subunits with the p85alpha regulatory subunit, impact of the His-tag on the catalytic activity, overview Homo sapiens

Protein Variants

Protein Variants Comment Organism
E545K site-directed mutagenesis of p110alpha, an oncogenic mutant enzyme form Homo sapiens
H1047R site-directed mutagenesis of p110alpha, an oncogenic mutant enzyme form Homo sapiens
additional information N-terminal tags on the catalytic (p110) subunit of phosphoinositol 3-kinase increase cell signalling and oncogenic transformation Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information Michaelis-Menten kinetics Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
110000
-
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate Homo sapiens
-
ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P27986 AND P42336 class Ia enzyme, subunits alpha and beta; class Ia enzyme
-
Homo sapiens P42338 AND O00329 class Ib enzyme, subunits alpha and beta; class Ib enzyme
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Homo sapiens ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
-
?

Subunits

Subunits Comment Organism
heterodimer 1* 85000, alpha-subunit, + 1 * 110000, beta-subunit Homo sapiens
More the heterodimers consisting of an 85 kDa regulatory/adapter subunit (p85) coupled to a 110 kDa catalytic subunit (p110) with both subunits possessing several isoforms Homo sapiens

Synonyms

Synonyms Comment Organism
phosphoinositol 3-kinase
-
Homo sapiens
PI 3-K
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
32
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

General Information

General Information Comment Organism
evolution class 1 phosphoinositide 3-kinases are heterodimers consisting of an 85 kDa regulatory/adapter subunit (p85) coupled to a 110 kDa catalytic subunit (p110) with both subunits possessing several isoforms. The class I enzymes are further subdivided into two subclasses: class Ia and class Ib. The class 1a phosphoinositol 3-kinases (p110alpha, p110beta and p110delta) signal downstream of tyrosine kinases, while the single class Ib phosphoinositol 3-kinase (p110gamma) operates downstream of heterotrimeric GPCRs (G-protein-coupled receptors) Homo sapiens
additional information N-terminal tags on the catalytic (p110) subunit of phosphoinositol 3-kinase increase cell signalling and oncogenic transformation, the increase in cell signalling and oncogenic-like transformation in response to p110 NTT is not mediated via an increase in the lipid kinase activity of the enzyme, but may be mediated by increased p110 autophosphorylation and/or other intracellular protein/protein interactions. Tagged recombinant protein is suitable for use in in vitro lipid kinase screens to identify phosphoinositol 3-kinase inhibitors, while in vivo (including intracellular) experiments and investigations into the protein kinase activity should be conducted with untagged constructs Homo sapiens