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Literature summary for 3.5.1.98 extracted from

  • Doyle, K.; Fitzpatrick, F.A.
    Redox signaling, alkylation (carbonylation) of conserved cysteines inactivates class I histone deacetylases 1, 2, and 3 and antagonizes their transcriptional repressor function (2010), J. Biol. Chem., 285, 17417-17424.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.98

Protein Variants

Protein Variants Comment Organism
C261S the single mutant forms about 70% less covalent adduct with 5-deoxy-DELTA12,14-prostaglandin J2-biotin compared to the wild type enzyme Homo sapiens
C261S/C273S the double mutant shows about 95% less alkylation by 0.005 mM 5-deoxy-DELTA12,14-prostaglandin J2-biotin compared to the wild type enzyme Homo sapiens
C273S the single mutant forms about 70% less covalent adduct with 5-deoxy-DELTA12,14-prostaglandin J2-biotin compared to the wild type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
15-deoxy-DELTA12,14-prostaglandin J2-biotin maximal inhibition of recombinant HDAC3 in complex with CoR1 is 50% Homo sapiens
4-hydroxy-2-nonenal maximal inhibition of recombinant HDAC3 in complex with CoR1 is 70% Homo sapiens
sodium butyrate
-
 Homo sapiens
trichostatin A
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
additional information cyclopentenone prostaglandins covalently alkylate (carbonylate) class I HDAC1, -2, and -3 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
HEK-293 cell
-
 Homo sapiens
-
HL-60 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylated histone + H2O
-
 Homo sapiens acetate + histone
-
 ?

Synonyms

Synonyms Comment Organism
class I histone deacetylase
-
 Homo sapiens
HDAC1
-
 Homo sapiens
HDAC2
-
 Homo sapiens
HDAC3
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.008
-
 recombinant HDAC3 in complex with CoR1, pH and temperature not specified in the publication Homo sapiens trichostatin A
0.013
-
 recombinant HDAC3 in complex with CoR1, pH and temperature not specified in the publication Homo sapiens sodium butyrate
0.098
-
 recombinant HDAC3 in complex with CoR1, pH and temperature not specified in the publication Homo sapiens 15-deoxy-DELTA12,14-prostaglandin J2-biotin
0.14
-
 recombinant HDAC3 in complex with CoR1, pH and temperature not specified in the publication Homo sapiens 4-hydroxy-2-nonenal

Expression

Organism Comment Expression
Homo sapiens redox signaling, alkylation (carbonylation) of conserved cysteines inactivates class I histone deacetylases 1, 2, and 3. Covalent modification at Cys261 and Cys273 in HDAC1, coincides with attenuation of histone deacetylase activity down

General Information

General Information Comment Organism
malfunction alkylation (carbonylation) of conserved cysteine residues in HDAC1, -2 and -3 antagonizes their deacetylase activity and transcriptional co-repressor function Homo sapiens