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Literature summary for 2.3.1.48 extracted from

  • Arif, M.; Pradhan, S.K.; Thanuja, G.R.; Vedamurthy, B.M.; Agrawal, S.; Dasgupta, D.; Kundu, T.K.
    Mechanism of p300 specific histone acetyltransferase inhibition by small molecules (2009), J. Med. Chem., 52, 267-277.
    View publication on PubMed
Search for more literature for 2.3.1.48

Inhibitors

Inhibitors Comment Organism Structure
garcinol competitive inhibitor versus both acetyl-CoA and histone, docking to the p300 HAT domain encompasses amino acid residues 1284-1673, and inhibition mechanism, overview. Also inhibits PCAF HAT activity, 90% inhibition at 0.04 mM Homo sapiens
isogarcinol competitive inhibitor versus both acetyl-CoA and histone, docking to the p300 HAT domain encompasses amino acid residues 1284-1673, and inhibition mechanism, overview. Also inhibits PCAF HAT activity to maximally 50% Homo sapiens
LTK14 noncompetitive inhibitor versus both acetyl-CoA and histone, docking to the p300 HAT domain encompasses amino acid residues 1284-1673, and inhibition mechanism, overview Homo sapiens
additional information effect of garcinol and its derivative on PCAF stability, overview. Isothermal titration calorimetry studies and molecular mechanisms of p300 HAT inhibition by specific and nonspecific HAT inhibitors: garcinol, isogarcinol. Residues LTK14, S1396, Y1397, G1626, and R1627 contact the inhibitors, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens mechanistically, p300 acts as a transcriptional coactivator through the direct interaction with a diverse set of transcription factors and RNA polymerase II transcription machinery ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q92831
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information mechanistically, p300 acts as a transcriptional coactivator through the direct interaction with a diverse set of transcription factors and RNA polymerase II transcription machinery Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
More functional domains of p300 include CH1, CH2, CH3, HAT domain, and Q/P-rich region, domain organization, overview Homo sapiens

Synonyms

Synonyms Comment Organism
HAT
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 Homo sapiens
p300
-
 Homo sapiens
P300/CBP-associated factor
-
 Homo sapiens
PCAF
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0039
-
 isogarcinol
-
 Homo sapiens
0.0049
-
 garcinol
-
 Homo sapiens
0.0051
-
 LTK14
-
 Homo sapiens

General Information

General Information Comment Organism
malfunction dysfunction of histone acetyltransferases leads to several diseases including cancer, diabetes, and asthma Homo sapiens
physiological function intrinsic HAT activity of p300 plays an important role in the transcriptional coactivation of CREB, c-Jun, c-Fos, c-Myb, p53, Stats, nuclear receptors, RelA GATA, p73, and others. The enzyme is involved in post-translational modifications of chromatin that play a key role in the regulation of gene expression, cell growth, and differentiation Homo sapiens