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Literature summary for 2.7.1.40 extracted from

  • Chaneton, B.; Hillmann, P.; Zheng, L.; Martin, A.C.; Maddocks, O.D.; Chokkathukalam, A.; Coyle, J.E.; Jankevics, A.; Holding, F.P.; Vousden, K.H.; Frezza, C.; OReilly, M.; Gottlieb, E.
    Serine is a natural ligand and allosteric activator of pyruvate kinase M2 (2012), Nature, 491, 458-462.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
fructose 1,6-bisphosphate activates isozyme PKM2 by direct binding Homo sapiens
L-serine allosteric activator of PKM2, activates isozyme PKM2 by direct binding Homo sapiens

Protein Variants

Protein Variants Comment Organism
H464A site-directed mutagenesis of isozyme PKM2, the mutant shows no binding of and activation by serine Homo sapiens
additional information construction of HCT116 cells silenced in both muscle isozymes PKM1 and PKM2, increased metabolic flux into the serine and glycine biosynthetic pathway in cells with reduced pyruvate kinase activity, serine and glycine deprivation decreases PKM2 activity in cells also influencing the glucose metabolism, overview Homo sapiens
S437Y site-directed mutagenesis of isozyme PKM2, the mutant shows no binding of and activation by fructose 1,6-bisphosphate Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information the absence of extracellular serine and glycine has a pronounced inhibitory effect on pyruvate kinase activity, and serine and glycine deprivation decreases PKM2 activity in cells Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Homo sapiens 5829
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + pyruvate Homo sapiens
-
 ADP + phosphoenolpyruvate
-
 r

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HCT-116 cell
-
 Homo sapiens
-
HT-29 cell
-
 Homo sapiens
-
additional information predominant isoform of pyruvate kinase in cancer cells is PKM2 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + pyruvate
-
 Homo sapiens ADP + phosphoenolpyruvate
-
 r

Synonyms

Synonyms Comment Organism
PKM2
-
 Homo sapiens
pyruvate kinase M2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

General Information

General Information Comment Organism
malfunction the absence of extracellular serine and glycine has a pronounced inhibitory effect on pyruvate kinase activity Homo sapiens
metabolism low pyruvate kinase activity can drive serine and glycine biosynthesis, important link between key metabolic processes observed in cancer, namely preferential PKM2 expression, aerobic glycolysis and serine biosynthesis Homo sapiens