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Literature summary extracted from

  • Jackson, M.D.; Schmidt, M.T.; Oppenheimer, N.J.; Denu, J.M.
    Mechanism of nicotinamide inhibition and transglycosidation by Sir2 histone/protein deacetylases (2003), J. Biol. Chem., 278, 50985-50998 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.286 3-acetylpyridine 16.8% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 3-bromopyridine 19.1% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 3-chloropyridine 9% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 3-fluoropyridine less than 2% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 3-hydroxypyridine 83.9% inhibition at 15 mM Saccharomyces cerevisiae
2.3.1.286 3-methoxypyridine 10.8% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 3-pyridine-carboxyaldehyde 10.6% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 3-Pyridinemethanol 22.5% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 nicotinamide noncompetitive inhibitor versus NAD+ Homo sapiens
2.3.1.286 nicotinamide noncompetitive inhibitor versus NAD+. 95% inhibition at 1.5 mM Saccharomyces cerevisiae
2.3.1.286 nicotinic acid 18.3% inhibition at 15 mM Saccharomyces cerevisiae
2.3.1.286 Pyridine 6.4% inhibition at 30 mM Saccharomyces cerevisiae
2.3.1.286 Thionicotinamide 58.3% inhibition at 15 mM Saccharomyces cerevisiae

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.286 [protein]-N6-acetyl-L-lysine + NAD+ + H2O Homo sapiens overall reaction [protein]-L-lysine + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
 ?
2.3.1.286 [protein]-N6-acetyl-L-lysine + NAD+ + H2O Saccharomyces cerevisiae overall reaction [protein]-L-lysine + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.286 Homo sapiens
-
-
-
2.3.1.286 Saccharomyces cerevisiae
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.286 KSTGGK(Ac)APRKQ + beta-2'-deoxy-2'-fluororibo-NAD+ + H2O the rates with beta-2'-deoxy-2'-fluororibo-NAD+ are about 200fold slower than the exchange rates determined with NAD+ under similar conditions Saccharomyces cerevisiae ?
-
 ?
2.3.1.286 KSTGGK(Ac)APRKQ + beta-2'-deoxy-2'-fluororibo-NAD+ + H2O the rates with beta-2'-deoxy-2'-fluororibo-NAD+ are about 1200fold slower than the exchange rates determined with NAD+ under similar conditions Homo sapiens ?
-
 ?
2.3.1.286 KSTGGK(Ac)APRKQ + NAD+ + H2O an 11-mer histone H3 peptide Homo sapiens KSTGGKAPRKQ + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
 ?
2.3.1.286 KSTGGK(Ac)APRKQ + NAD+ + H2O an 11-mer histone H3 peptide Saccharomyces cerevisiae KSTGGKAPRKQ + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
 ?
2.3.1.286 [protein]-N6-acetyl-L-lysine + NAD+ + H2O overall reaction Homo sapiens [protein]-L-lysine + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
 ?
2.3.1.286 [protein]-N6-acetyl-L-lysine + NAD+ + H2O overall reaction Saccharomyces cerevisiae [protein]-L-lysine + 2''-O-acetyl-ADP-D-ribose + nicotinamide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.286 HST2
-
 Saccharomyces cerevisiae
2.3.1.286 silent information regulator 2
-
 Homo sapiens
2.3.1.286 silent information regulator 2
-
 Saccharomyces cerevisiae
2.3.1.286 Sir2
-
 Homo sapiens
2.3.1.286 Sir2
-
 Saccharomyces cerevisiae
2.3.1.286 SIRT2
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.3.1.286 NAD+
-
 Homo sapiens
2.3.1.286 NAD+
-
 Saccharomyces cerevisiae

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.1.286 0.0339
-
 nicotinamide at pH 7.5 and 37°C Homo sapiens
2.3.1.286 0.298
-
 nicotinamide at pH 7.5 and 37°C Saccharomyces cerevisiae