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Literature summary for 2.3.1.286 extracted from

  • Smith, B.C.; Denu, J.M.
    Mechanism-based inhibition of Sir2 deacetylases by thioacetyl-lysine peptide (2007), Biochemistry, 46, 14478-14486 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
[histone H3]-difluoroacetyl-L-lysine
-
Homo sapiens
[histone H3]-difluoroacetyl-L-lysine
-
Saccharomyces cerevisiae
[histone H3]-monofluoroacetyl-L-lysine
-
Homo sapiens
[histone H3]-monofluoroacetyl-L-lysine
-
Saccharomyces cerevisiae
[histone H3]-thioacetyl-L-lysine most potent inhibitor Homo sapiens
[histone H3]-thioacetyl-L-lysine most potent inhibitor Saccharomyces cerevisiae
[histone H3]-trifluoroacetyl-L-lysine
-
Homo sapiens
[histone H3]-trifluoroacetyl-L-lysine
-
Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Saccharomyces cerevisiae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
[histone H3]-N6-acetyl-L-lysine + NAD+ + H2O
-
Homo sapiens [histone H3]-L-lysine + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
?
[histone H3]-N6-acetyl-L-lysine + NAD+ + H2O
-
Saccharomyces cerevisiae [histone H3]-L-lysine + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
?

Synonyms

Synonyms Comment Organism
HST2
-
Saccharomyces cerevisiae
Sir2
-
Homo sapiens
Sir2
-
Saccharomyces cerevisiae
SIRT1
-
Homo sapiens
SIRT2
-
Homo sapiens
SIRT3
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+
-
Homo sapiens
NAD+
-
Saccharomyces cerevisiae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00102
-
at pH 7.5 and 25°C Saccharomyces cerevisiae [histone H3]-thioacetyl-L-lysine
0.061
-
at pH 7.5 and 25°C Saccharomyces cerevisiae [histone H3]-trifluoroacetyl-L-lysine
0.132
-
at pH 7.5 and 25°C Saccharomyces cerevisiae [histone H3]-difluoroacetyl-L-lysine
0.133
-
at pH 7.5 and 25°C Saccharomyces cerevisiae [histone H3]-monofluoroacetyl-L-lysine