BRENDA - Enzyme Database show

Mechanism of inhibition of the human sirtuin enzyme SIRT3 by nicotinamide: computational and experimental studies

Guan, X.; Lin, P.; Knoll, E.; Chakrabarti, R.; PLoS One 15, e107729 (2014)

Data extracted from this reference:

Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.3.1.286
Isonicotinamide
weak competitive inhibitor of hSIRT3 with respect to NAD+ in vitro; weak inhibitor
Homo sapiens
2.3.1.286
nicotinamide
mixed noncompetitive inhibitor. Inhibition of SIRT3 involves apparent competition between the inhibitor and the enzyme cofactor NAD+; predominantly noncompetitive inhibitor
Homo sapiens
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.3.1.286
Homo sapiens
Q96EB6
-
-
2.3.1.286
Homo sapiens
Q9NTG7
-
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.3.1.286
NAD+ + TRSG(N6-acetyl)KVMRRLLR
acetylated substrate peptide based on the sequence of acetyl-coenzyme A synthetase 2
730679
Homo sapiens
nicotinamide + TRSGKVMRRLLR + 2'-O-acetyl-ADP-ribose
-
-
-
?
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.3.1.286
0.0367
-
pH 8, 37°C
Homo sapiens
nicotinamide
2.3.1.286
0.0681
-
pH 8, 37°C
Homo sapiens
nicotinamide
2.3.1.286
12200
-
pH 8, 37°C, weak inhibitor
Homo sapiens
Isonicotinamide
2.3.1.286
13800
-
pH 8, 37°C, weak competitive inhibitor of hSIRT3 with respect to NAD+ in vitro
Homo sapiens
Isonicotinamide
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.3.1.286
0.0367
-
pH 8, 37°C
Homo sapiens
nicotinamide
2.3.1.286
0.0681
-
pH 8, 37°C
Homo sapiens
nicotinamide
2.3.1.286
12200
-
pH 8, 37°C, weak inhibitor
Homo sapiens
Isonicotinamide
2.3.1.286
13800
-
pH 8, 37°C, weak competitive inhibitor of hSIRT3 with respect to NAD+ in vitro
Homo sapiens
Isonicotinamide
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.3.1.286
Isonicotinamide
weak inhibitor
Homo sapiens
2.3.1.286
Isonicotinamide
weak competitive inhibitor of hSIRT3 with respect to NAD+ in vitro
Homo sapiens
2.3.1.286
nicotinamide
predominantly noncompetitive inhibitor
Homo sapiens
2.3.1.286
nicotinamide
mixed noncompetitive inhibitor. Inhibition of SIRT3 involves apparent competition between the inhibitor and the enzyme cofactor NAD+
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.3.1.286
NAD+ + TRSG(N6-acetyl)KVMRRLLR
acetylated substrate peptide based on the sequence of acetyl-coenzyme A synthetase 2
730679
Homo sapiens
nicotinamide + TRSGKVMRRLLR + 2'-O-acetyl-ADP-ribose
-
-
-
?