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Literature summary for 3.5.1.98 extracted from

  • Weerasinghe, S.V.; Estiu, G.; Wiest, O.; Pflum, M.K.
    Residues in the 11 A channel of histone deacetylase 1 promote catalytic activity: implications for designing isoform-selective histone deacetylase inhibitors (2008), J. Med. Chem., 51, 5542-5551.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine because of their fundamental role in gene expression, histone deacetylase proteins are promising targets for cancer treatment Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
HDAC1 mutants are cloned into pBJ5HDAC1-F Homo sapiens

Protein Variants

Protein Variants Comment Organism
D99A mutated channel residue, 25% deacetylase activity Homo sapiens
E98A mutated channel residue, 120% deacetylase activity Homo sapiens
F150A mutated channel residue, 12% deacetylase activity Homo sapiens
F205A mutated channel residue, 20% deacetylase activity Homo sapiens
G149A mutated channel residue, 10% deacetylase activity Homo sapiens
H141A mutated channel residue, 20% deacetylase activity Homo sapiens
H28A mutated channel residue, 20% deacetylase activity Homo sapiens
L271A mutated channel residue, 12% deacetylase activity Homo sapiens
P29A mutated channel residue, 18% deacetylase activity Homo sapiens
Y204A mutated channel residue, 40% deacetylase activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
MS-275
-
Homo sapiens
suberoylanilide hydroxamic acid SAHA, vorinostat Homo sapiens
trichostatin A TSA Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.066
-
Fluor de Lys HDAC substrate mutant F150A Homo sapiens
0.088
-
Fluor de Lys HDAC substrate wild type Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens histone deacetylase proteins catalyze the removal of acetyl groups from acetylated lysines on histone substrates ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q13547
-
-

Source Tissue

Source Tissue Comment Organism Textmining
JURKAT cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Fluor de Lys HDAC substrate + H2O
-
Homo sapiens ?
-
?
additional information histone deacetylase proteins catalyze the removal of acetyl groups from acetylated lysines on histone substrates Homo sapiens ?
-
?
additional information Fluor de Lys HDAC substrate, commercially available kit Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
histone deacetylase 1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
activity assay Homo sapiens