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Literature summary extracted from

  • Johnson, L.N.; Noble, M.E.M.; Owen, D.J.
    Active and inactive protein kinases: structural basis for regulation (1996), Cell, 85, 149-158.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.11 cAMP required for activity, activation is mediated by binding of cAMP to the regulatory subunits, causing release of the catalytic subunits Mammalia
2.7.11.19 additional information activation segment structure Mammalia
2.7.11.22 cyclin dependent on, forms complexes with cyclin A Homo sapiens
2.7.11.24 additional information phosphorylation at Thr183 and Tyr185 activates the enzyme Mammalia

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.11.11 crystallization in active conformation Mammalia
2.7.11.19 crystallization of PhK in active conformation Mammalia

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.11 adenosine 5'-(beta,gamma-Imino)triphosphate binding structure at the ATP binding site Mammalia
2.7.11.17 additional information autoinhibitory, in absence of Ca2+/calmodulin the enzyme shows an open conformation with extensive interactions between the C-terminal autoinhibitory sequence and the kinase core influencing the binding site for ATP Mammalia

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.11 cytoplasm primarily, enzyme can migrate to the nucleus upon activation Mammalia 5737
-
2.7.11.11 nucleus enzyme can migrate from the cytoplasm to the nucleus upon activation Mammalia 5634
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.11 Mg2+ activates the enzyme, binds to beta- and gamma-phosphate of ATP and to Asp184 Mammalia
2.7.11.17 Ca2+ binding required for activity Mammalia
2.7.11.19 Mg2+
-
 Mammalia
2.7.11.22 Mg2+
-
 Homo sapiens
2.7.11.24 Mg2+
-
 Mammalia

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.11 ATP + a protein Mammalia the enzyme is a key player in cellular responses to the second messenger cAMP ADP + a phosphoprotein
-
 ?
2.7.11.17 ATP + a protein Mammalia the enzyme phosphorylates e.g. the synaptic vesicle-associated protein synapsin 1 and synapsin 2 ADP + a phosphoprotein
-
 ?
2.7.11.19 ATP + phosphorylase b Mammalia
-
 ADP + phosphorylase a
-
 ?
2.7.11.22 ATP + a protein Homo sapiens
-
 ADP + a phosphoprotein
-
 ?
2.7.11.24 ATP + a protein Mammalia
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.11 Mammalia
-
-
-
2.7.11.17 Mammalia
-
-
-
2.7.11.19 Mammalia
-
-
-
2.7.11.22 Homo sapiens
-
-
-
2.7.11.24 Mammalia
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.11 phosphoprotein autophosphorylation at Thr197 required for activation Mammalia
2.7.11.17 phosphoprotein phosphorylation at Thr177 in the activation segment leads to activation Mammalia
2.7.11.22 phosphoprotein phosphorylation at Thr160 leads to inactivation and closed conformation Homo sapiens
2.7.11.24 phosphoprotein phosphorylation at Thr183 and Tyr185 for activation Mammalia

Reaction

EC Number Reaction Comment Organism Reaction ID
2.7.11.11 ATP + a [protein]-(L-serine/L-threonine) = ADP + a [protein]-(L-serine/L-threonine) phosphate catalytic site structure, Asp166 is the catalytic base invariant in all kinases, activation mechanism, overview Mammalia
a
2.7.11.17 ATP + a [protein]-(L-serine/L-threonine) = ADP + a [protein]-(L-serine/L-threonine) phosphate catalytic aspartate residue Mammalia
a
2.7.11.19 2 ATP + phosphorylase b = 2 ADP + phosphorylase a catalytic aspartate residue Mammalia
a
2.7.11.22 ATP + a [protein]-(L-serine/L-threonine) = ADP + a [protein]-(L-serine/L-threonine) phosphate catalytic aspartate residue Homo sapiens
a
2.7.11.24 ATP + a [protein]-(L-serine/L-threonine) = ADP + a [protein]-(L-serine/L-threonine) phosphate catalytic aspartate residue Mammalia
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.11 ATP + a protein the enzyme is a key player in cellular responses to the second messenger cAMP Mammalia ADP + a phosphoprotein
-
 ?
2.7.11.11 ATP + a protein phosphorylates nuclear proteins important for gene replication Mammalia ADP + a phosphoprotein
-
 ?
2.7.11.17 ATP + a protein
-
 Mammalia ADP + a phosphoprotein
-
 ?
2.7.11.17 ATP + a protein the enzyme phosphorylates e.g. the synaptic vesicle-associated protein synapsin 1 and synapsin 2 Mammalia ADP + a phosphoprotein
-
 ?
2.7.11.19 ATP + phosphorylase b
-
 Mammalia ADP + phosphorylase a
-
 ?
2.7.11.22 ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?
2.7.11.24 ATP + a protein
-
 Mammalia ADP + a phosphoprotein
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.11 More the enzyme possesses a regulatory and a catalytic subunit, 2 lobes are comprised in the core scaffold, the N-terminal beta-sheet and C-terminal alpha-helix lobe, which are joined by a polypeptide chain, the active is located at the interface of the 2 lobes Mammalia
2.7.11.11 tetramer alpha2beta2, the tetramer is inactive, binding of ATP causes release of the 2 catalytic subunits in active conformation Mammalia
2.7.11.17 More the enzyme has an open, active conformation and a closed, inactive conformation Mammalia
2.7.11.19 More the enzyme has an open, active conformation and a closed, inactive conformation Mammalia
2.7.11.22 More the enzyme has an open, active conformation and a closed, inactive conformation Homo sapiens
2.7.11.24 More the enzyme has an open, active conformation and a closed, inactive conformation Mammalia

Synonyms

EC Number Synonyms Comment Organism
2.7.11.11 cAPK
-
 Mammalia
2.7.11.11 cyclic AMP-dependent kinase
-
 Mammalia
2.7.11.17 CaMKI
-
 Mammalia
2.7.11.19 PhK
-
 Mammalia
2.7.11.22 CDK2
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.11 ATP binding site structure: spans both lobes, the N-terminal beta-sheet and C-terminal alpha-helix of the core scaffold, binding of ATP and release of ADP in the open enzyme conformation, residues Asp184, Lys72, and Asp166 are involved, schematic overview Mammalia
2.7.11.17 ATP the ATP-binding site is influenced by the autoinhibitory conformation Mammalia
2.7.11.17 Calmodulin binding required for activity Mammalia
2.7.11.19 ATP
-
 Mammalia
2.7.11.22 ATP
-
 Homo sapiens
2.7.11.24 ATP
-
 Mammalia