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Literature summary for 3.5.1.98 extracted from

  • Nian, H.; Bisson, W.H.; Dashwood, W.M.; Pinto, J.T.; Dashwood, R.H.
    Alpha-keto acid metabolites of organoselenium compounds inhibit histone deacetylase activity in human colon cancer cells (2009), Carcinogenesis, 30, 1416-1423.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
alpha-keto-gamma-methylselenobutyrate causes dose-dependent inhibition of HDAC activity, HDAC1 shows about 80% residual activity at 2 mM, HDAC8 shows less than 60% residual activity at 2 mM Homo sapiens
beta-methylselenopyruvate causes dose-dependent inhibition of HDAC activity, competitive inhibitor of HDAC8, HDAC1 shows about 30% residual activity at 2 mM, HDAC8 shows less than 30% residual activity at 2 mM Homo sapiens
Butyrate
-
Homo sapiens
additional information methylselenocysteine and selenomethionine have little or no inhibitory activity up to 2 mM Homo sapiens

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BY41
-
-

Source Tissue

Source Tissue Comment Organism Textmining
colonic cancer cell
-
Homo sapiens
-
HCT-116 cell
-
Homo sapiens
-
HT-29 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-acetyl-lysine-histone H3 + H2O
-
Homo sapiens acetate + histone H3
-
?

Synonyms

Synonyms Comment Organism
HDAC1
-
Homo sapiens
HDAC8
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.02
-
HDAC8, at 37°C, pH not specified in the publication Homo sapiens beta-methylselenopyruvate