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Literature summary for 2.7.11.11 extracted from

  • Adams Joseph, A.
    Activation loop phosphorylation and catalysis in protein kinases: is there functional evidence for the autoinhibitor model? (2003), Biochemistry, 42, 601-607.
    View publication on PubMed
Search for more literature for 2.7.11.11

Activating Compound

Activating Compound Comment Organism Structure
cAMP
-
 eukaryota
additional information activation involves the activation loop, a polypeptide region outside the active site cleft, which is reversibly phosphorylated at Thr197, dephosphorylation leads to enzyme activation by 2-3fold eukaryota

Crystallization (Commentary)

Crystallization (Comment) Organism
X-ray diffraction structure analysis eukaryota

Protein Variants

Protein Variants Comment Organism
T197A site-directed mutagenesis, highly reduced activity compared to the wild-type enzyme eukaryota
T197D site-directed mutagenesis, reduced activity compared to the wild-type enzyme eukaryota

Inhibitors

Inhibitors Comment Organism Structure
additional information phosphorylation of the activation loop leads to enzyme inhibition, in which the phosphorylated activation loop acts as an autoinhibitory substrate blocking the nucleotide binding pocket, competition with ATP eukaryota

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information kinetics of activation and autoinhibition, modeling, pre-steady-state kinetic methods, wild-type and mutant enzymes eukaryota

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 eukaryota

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a protein eukaryota regulation by reversible phosphorylation, overview ADP + a phosphoprotein
-
 ?

Organism

Organism UniProt Comment Textmining
eukaryota
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein the enzyme is regulated by reversible phosphorylation of the activation loop at Thr197, a polypeptide region outside the active site cleft, the enzyme is inhibited by phosphorylation, which also increases the affinity for ATP by 2fold, and activated by dephosphorylation eukaryota

Reaction

Reaction Comment Organism Reaction ID
ATP + a [protein]-(L-serine/L-threonine) = ADP + a [protein]-(L-serine/L-threonine) phosphate activation involves the activation loop, a polypeptide region outside the active site cleft, which is reversibly phosphorylated at Thr197, phosphorylation leads to enzyme inhibition, activation mechanism, overview eukaryota
a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
 eukaryota ADP + a phosphoprotein
-
 ?
ATP + a protein regulation by reversible phosphorylation, overview eukaryota ADP + a phosphoprotein
-
 ?

Synonyms

Synonyms Comment Organism
cAMP-dependent protein kinase
-
 eukaryota
PKA
-
 eukaryota

Cofactor

Cofactor Comment Organism Structure
ATP the binding site is a deep pocket lined by hydrophobic residues, enzyme affinity for ATP is increased 2fold by phosphorylation of the activation loop at Thr197, ATP competes with the phosphorylated activation loop, that acts as an autoinhibitory substrate eukaryota