Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.3.1.48 extracted from

  • Secci, D.; Carradori, S.; Bizzarri, B.; Bolasco, A.; Ballario, P.; Patramani, Z.; Fragapane, P.; Vernarecci, S.; Canzonetta, C.; Filetici, P.
    Synthesis of a novel series of thiazole-based histone acetyltransferase inhibitors (2014), Bioorg. Med. Chem., 22, 1680-1689.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(4-(4-chlorophenyl)thiazol-2-yl)-2-(propan-2-ylidene)hydrazine i.e. BF1, shows substrate selectivity for histone H3 acetylation and inhibitory activity in vitro on recombinant HATs Gcn5 and p300. Both global acetylation of histone H3 and specific acetylation at lysine 18 (H3AcK18) are lowered by BF1 treatment Homo sapiens
1-(4-(4-chlorophenyl)thiazol-2-yl)-2-(propan-2-ylidene)hydrazine i.e. BF1, shows substrate selectivity for histone H3 acetylation and inhibitory activity in vitro on recombinant HATs Gcn5 and p300. Both global acetylation of histone H3 and specific acetylation at lysine 18 (H3AcK18) are lowered by BF1 treatment Saccharomyces cerevisiae
additional information synthesis of a novel series of thiazole-based histone acetyltransferase inhibitors active both in vitro and in vivo, overview Homo sapiens
additional information synthesis of a novel series of thiazole-based histone acetyltransferase inhibitors active both in vitro and in vivo, overview Saccharomyces cerevisiae

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
Homo sapiens 5634
-
nucleus
-
Saccharomyces cerevisiae 5634
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acetyl-CoA + histone Homo sapiens
-
CoA + acetylhistone
-
?
acetyl-CoA + histone Saccharomyces cerevisiae
-
CoA + acetylhistone
-
?
acetyl-CoA + histone H3 Homo sapiens acetylation at Lys18 CoA + acetylhistone H3
-
?
acetyl-CoA + histone H3 Saccharomyces cerevisiae acetylation at Lys18 CoA + acetylhistone H3
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Saccharomyces cerevisiae
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
glioblastoma cell from brain tumor Homo sapiens
-
HeLa cell
-
Homo sapiens
-
neuroblastoma cell from neuronal tissue Homo sapiens
-
SK-N-BE(2) cell
-
Homo sapiens
-
U-87 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + histone
-
Homo sapiens CoA + acetylhistone
-
?
acetyl-CoA + histone
-
Saccharomyces cerevisiae CoA + acetylhistone
-
?
acetyl-CoA + histone H3 acetylation at Lys18 Homo sapiens CoA + acetylhistone H3
-
?
acetyl-CoA + histone H3 acetylation at Lys18 Saccharomyces cerevisiae CoA + acetylhistone H3
-
?

Synonyms

Synonyms Comment Organism
HAT
-
Homo sapiens
HAT
-
Saccharomyces cerevisiae

General Information

General Information Comment Organism
evolution acetyltransferases are very well conserved through evolution Homo sapiens
evolution acetyltransferases are very well conserved through evolution Saccharomyces cerevisiae
metabolism acetylation, which targets a broad range of histone and non-histone proteins, is a reversible mechanism and plays a critical role in eukaryotic genes activation/deactivation Homo sapiens
metabolism acetylation, which targets a broad range of histone and non-histone proteins, is a reversible mechanism and plays a critical role in eukaryotic genes activation/deactivation Saccharomyces cerevisiae