Literature summary for 2.7.1.40 extracted from

Matsuda, S.; Adachi, J.; Ihara, M.; Tanuma, N.; Shima, H.; Kakizuka, A.; Ikura, M.; Ikura, T.; Matsuda, T.
Nuclear pyruvate kinase M2 complex serves as a transcriptional coactivator of arylhydrocarbon receptor (2016), Nucleic Acids Res., 44, 636-647 .

Search for more literature for 2.7.1.40

Activating Compound

Activating Compound	Comment	Organism	Structure
fructose 1,6-bisphosphate	FBP, enzyme PKM2 is allosterically activated by the glycolytic metabolite	Homo sapiens

Cloned(Commentary)

Cloned (Comment)	Organism
gene PKM2, PKM2 overexpression in Hep-G2 cells, real-time RT-PCR enzyme expression analysis, recombinant overexpression of wild-type PKM2 and PKM2 K367M mutant in PKM2-knockdown HeLa S3 cells	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
K367M	site-directed mutagenesis, the mutant lacks pyruvate kinase activity	Homo sapiens
additional information	PKM2 knockout, retroviral production is used to generate HeLa S3 cells stably expressing shRNAs specific for PKM2 or AhR, and stable clones are selected with puromycin	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
nucleus	PKM2, PDC-E2, and p300 constitute a complex with AhR on chromatin. PKM2 is recruited to gene enhancers of the AhR-target genes in an AhR-dependent manner	Homo sapiens	5634	-

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.
ADP + phosphoenolpyruvate	Homo sapiens	-	ATP + pyruvate	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P14618	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
HeLa-S3 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

General Information

General Information	Comment	Organism
malfunction	overexpression of wild-type PKM2 increases H3K9 acetylation at the CYP1A1 enhancer, whereas overexpression of the PKM2K367M mutant fails to do so, indicating that efficient histone acetylation at the CYP1A1 enhancer requires the pyruvate kinase activity of PKM2	Homo sapiens
metabolism	pyruvate kinase M2 (PKM2) and pyruvate dehydrogenase complex (PDC) regulate production of acetyl-CoA, which functions as an acetyl donor in diverse enzymatic reactions, including histone acetylation. PKM2, the E2 subunit of PDC and histone acetyltransferase p300 constitute a complex on chromatin with arylhydrocarbon receptor (AhR), a transcription factor associated with xenobiotic metabolism. All of these factors are recruited to the enhancer of AhR-target genes, in an AhR-dependent manner	Homo sapiens
physiological function	PKM2 is recruited to gene enhancers of the AhR-target genes in an AhR-dependent manner and promotes AhR transactivation. Pyruvate kinase M2 (PKM2) and pyruvate dehydrogenase complex (PDC) regulate production of acetyl-CoA, which functions as an acetyl donor in diverse enzymatic reactions, including histone acetylation. PKM2, the E2 subunit of PDC and histone acetyltransferase p300 constitute a complex on chromatin with arylhydrocarbon receptor (AhR), a transcription factor associated with xenobiotic metabolism. All of these factors, also PKM2, are recruited to the enhancer of AhR-target genes, in an AhR-dependent manner. PKM2 contributes to enhancement of transcription of cytochrome P450 1A1 (CYP1A1), an AhR-target gene, acetylation at lysine 9 of histone H3 at the CYP1A1 enhancer. A local acetyl-CoA production system is proposed in which PKM2 and PDC locally supply acetyl-CoA to p300 from abundant PEP for histone acetylation at the gene enhancer. PKM2 sensitizes AhR-mediated detoxification in actively proliferating cells such as cancer and fetal cells	Homo sapiens

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Release 2023.1 (January 2023)