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Literature summary for 2.3.1.48 extracted from

  • Milite, C.; Castellano, S.; Benedetti, R.; Tosco, A.; Ciliberti, C.; Vicidomini, C.; Boully, L.; Franci, G.; Altucci, L.; Mai, A.; Sbardella, G.
    Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs) (2011), Bioorg. Med. Chem., 19, 3690-3701.
    View publication on PubMed
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Activating Compound

Activating Compound Comment Organism Structure
2-dodecylmalonate compound induces hyperacetylation of specific lysine residues of histone H3, in particular residues K9 and K18, and raises the level of pan-acetylated H4. Compound inhibits the acetylation of all the other H3 and H4 lysines, with the exception of residue K8Ac of histone H4 Homo sapiens
diethyl 2-pentadecylidenemalonate compound induces hyperacetylation of specific lysine residues of histone H3, in particular residues K9 and K18, and raises the level of pan-acetylated H4 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-dodecylmalonate compound induces hyperacetylation of specific lysine residues of histone H3, in particular residues K9 and K18, and raises the level of pan-acetylated H4. Compound inhibits the acetylation of all the other H3 and H4 lysines, with the exception of residue K8Ac of histone H4 Homo sapiens
2-tridecylmalonate inhibition of the acetylation of histone H3 residuesK9/K18, being practically inactive in all the other assays Homo sapiens
2-undecylmalonate compound exhibits a significant inhibition of the acetylation of almost any lysine residue explored, with the sole exception of residue K8 of H4. Compound reduces the level of K5Ac of H4 and, more markedly, K16Ac of H4 Homo sapiens
3-pentadecylidenepentane-2,4-dione inhibition of the acetylation of histone H3 residuesK9/K14, being practically inactive in all the other assays Homo sapiens
diethyl 2-tetradecylidenemalonate compound exhibits a significant inhibition of the acetylation of almost any lysine residue explored, with the sole exception of residue K8 of H4. Compound reduces the level of K5Ac of H4 and, more markedly, K16Ac of H4 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
U-937 cell
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 Homo sapiens
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