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Literature summary for 2.7.1.40 extracted from

  • Spoden, G.A.; Mazurek, S.; Morandell, D.; Bacher, N.; Ausserlechner, M.J.; Jansen-Duerr, P.; Eigenbrodt, E.; Zwerschke, W.
    Isotype-specific inhibitors of the glycolytic key regulator pyruvate kinase subtype M2 moderately decelerate tumor cell proliferation (2008), Int. J. Cancer, 123, 312-321.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
EGMVLPTVWQPANWMCRLSN peptide aptamer placed within thioredoxin A. Aptamer specifically binds to M2 pyruvate kinase and shifts the isoenzyme into its low affinity dimeric conformation Homo sapiens
EGQLRHWGWAWSLASQNFSI peptide aptamer placed within thioredoxin A. Aptamer specifically binds to M2 pyruvate kinase and shifts the isoenzyme into its low affinity dimeric conformation Homo sapiens
additional information screen of a galactose-inducible combinatorial peptide aptamer library consisting of specific 20-mer peptides placed within 12-kDa protein thioredoxin A identifies 14 aptamers which specifically bind to M2 pyruvate kinase and shift the isoenzyme into its low affinity dimeric conformation. The aptamer-induced dimerization and inactivation of M2 pyruvate kinase leads to a significant decrease in the pyruvate kinase mass-action ratio as well as ATP:ADP ratio in the target cells. The expression of M2-pyruvate kinase-binding peptide aptamers moderately reduces the growth of immortalized NIH3T3 cell populations by decelerating cell proliferation, but without affecting apoptotic cell death. The M2-PK-binding peptide aptamers also reduce the proliferation rate of human U-2 OS osteosarcoma cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
U2-OS cell
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Homo sapiens
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