BRENDA - Enzyme Database show

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis

Hasmann, M.; Schemainda, I.; Cancer Res. 63, 7436-7442 (2003)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
2.4.2.12
pharmacology
enzyme is a potential target for development of anticancer drugs
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.4.2.12
FK866
a highly specific noncompetitive inhibitor the enzyme, represents a novel mechanism for induction of tumor cell apoptosis, counteracted by nicotinic acid and nicotinamide
Homo sapiens
Localization
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
2.4.2.12
mitochondrion
-
Homo sapiens
5739
-
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.4.2.12
additional information
Homo sapiens
FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+
?
-
-
-
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
Homo sapiens
key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide
nicotinamide D-ribonucleotide + diphosphate
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.4.2.12
Homo sapiens
-
-
-
Purification (Commentary)
EC Number
Commentary
Organism
2.4.2.12
partially frim K-562 leukemic cells
Homo sapiens
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
2.4.2.12
Hep-G2 cell
liver carcinoma cell line
Homo sapiens
-
2.4.2.12
K-562 cell
leukemia cell line
Homo sapiens
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.4.2.12
additional information
FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+
661421
Homo sapiens
?
-
-
-
-
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
661421
Homo sapiens
nicotinamide D-ribonucleotide + diphosphate
-
-
-
?
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide
661421
Homo sapiens
nicotinamide D-ribonucleotide + diphosphate
-
-
-
?
Temperature Optimum [°C]
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
2.4.2.12
37
-
assay at
Homo sapiens
pH Optimum
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
2.4.2.12
8.8
-
assay at
Homo sapiens
Ki Value [mM]
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
2.4.2.12
0.0003
-
FK866
free enzyme
Homo sapiens
2.4.2.12
0.0004
-
FK866
enzyme-substrate complex
Homo sapiens
Application (protein specific)
EC Number
Application
Commentary
Organism
2.4.2.12
pharmacology
enzyme is a potential target for development of anticancer drugs
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.4.2.12
FK866
a highly specific noncompetitive inhibitor the enzyme, represents a novel mechanism for induction of tumor cell apoptosis, counteracted by nicotinic acid and nicotinamide
Homo sapiens
Ki Value [mM] (protein specific)
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
2.4.2.12
0.0003
-
FK866
free enzyme
Homo sapiens
2.4.2.12
0.0004
-
FK866
enzyme-substrate complex
Homo sapiens
Localization (protein specific)
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
2.4.2.12
mitochondrion
-
Homo sapiens
5739
-
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.4.2.12
additional information
Homo sapiens
FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+
?
-
-
-
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
Homo sapiens
key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide
nicotinamide D-ribonucleotide + diphosphate
-
-
?
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
2.4.2.12
partially frim K-562 leukemic cells
Homo sapiens
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
2.4.2.12
Hep-G2 cell
liver carcinoma cell line
Homo sapiens
-
2.4.2.12
K-562 cell
leukemia cell line
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.4.2.12
additional information
FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+
661421
Homo sapiens
?
-
-
-
-
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
661421
Homo sapiens
nicotinamide D-ribonucleotide + diphosphate
-
-
-
?
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide
661421
Homo sapiens
nicotinamide D-ribonucleotide + diphosphate
-
-
-
?
Temperature Optimum [°C] (protein specific)
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
2.4.2.12
37
-
assay at
Homo sapiens
pH Optimum (protein specific)
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
2.4.2.12
8.8
-
assay at
Homo sapiens