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Literature summary for 3.5.1.98 extracted from

  • Dowling, D.P.; Gantt, S.L.; Gattis, S.G.; Fierke, C.A.; Christianson, D.W.
    Structural studies of human histone deacetylase 8 and its site-specific variants complexed with substrate and inhibitors (2008), Biochemistry, 47, 13554-13563.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.98

Cloned(Commentary)

Cloned (Comment) Organism
a pET20b-derived HDAC8-His expression plasmid with optimized codon usage, pHD2-His, is modified to add a factor Xa cleavage site, generating pHD2-Xa-His Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
seven structures of wild-type HDAC8 and mutants in complex with inhibitors or substrate are determined to a resolution of 1.8 to 3.3 A Homo sapiens

Protein Variants

Protein Variants Comment Organism
D101A mutant, confirms that the strictly conserved side chain of D101 is crucial for the function of the L2 loop Homo sapiens
D101E mutant, confirms that the strictly conserved side chain of D101 is crucial for the function of the L2 loop Homo sapiens
D101L mutant, confirms that the strictly conserved side chain of D101 is crucial for the function of the L2 loop Homo sapiens
D101N mutant, confirms that the strictly conserved side chain of D101 is crucial for the function of the L2 loop Homo sapiens
H143A mutant, the substitution abolishes enzyme activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide APHA Homo sapiens
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide M344 Homo sapiens
suberoylanilide hydroxamic acid SAHA Homo sapiens
trichostatin A TSA Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.14
-
 Fluor de Lys HDAC8 substrate Co2+-D101E mutant Homo sapiens
0.16
-
 Fluor de Lys HDAC8 substrate Co2+-wild type Homo sapiens
1
-
 Fluor de Lys HDAC8 substrate Co2+-D101A mutant, larger than 1.00 Homo sapiens
1
-
 Fluor de Lys HDAC8 substrate Co2+-D101L mutant, larger than 1.00 Homo sapiens
1
-
 Fluor de Lys HDAC8 substrate Co2+-D101N mutant, larger than 1.00 Homo sapiens
1
-
 Fluor de Lys HDAC8 substrate Co2+-H143A mutant, larger than 1.00 Homo sapiens
1.1
-
 Fluor de Lys HDAC8 substrate Zn2+-wild type Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+
-
 Homo sapiens
Fe2+
-
 Homo sapiens
Zn2+
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BY41
-
-

Purification (Commentary)

Purification (Comment) Organism
proteins are expressed in Escherichia coli BL21DE3 cells and purified using nickel nitrilotriacetic acid or TALON affinity resin, a GE HiTrap Q HP and a Superdex 26-60 column Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Fluor de Lys HDAC8 substrate + H2O commercially available kit Homo sapiens ?
-
 ?
N-acetyl-arginine-histidine-acetyl-lysine-acetyl-lysine-coumarin + H2O substrate in crystallized enzyme-substrate complex Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
histone deacetylase 8
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 activity assay Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.15
-
 Fluor de Lys HDAC8 substrate Co2+-D101E mutant Homo sapiens
0.9
-
 Fluor de Lys HDAC8 substrate Zn2+-wild type Homo sapiens
1.2
-
 Fluor de Lys HDAC8 substrate Co2+-wild type Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 activity assay Homo sapiens