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Literature summary 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

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

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.5.1.98 0.066
-
 Fluor de Lys HDAC substrate mutant F150A Homo sapiens
3.5.1.98 0.088
-
 Fluor de Lys HDAC substrate wild type Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.5.1.98 Homo sapiens Q13547
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.5.1.98 JURKAT cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
3.5.1.98 histone deacetylase 1
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.5.1.98 37
-
 activity assay Homo sapiens