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Literature summary for 2.4.2.12 extracted from

  • Hasmann, M.; Schemainda, I.
    FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis (2003), Cancer Res., 63, 7436-7442.
    View publication on PubMed

Application

Application Comment Organism
pharmacology enzyme is a potential target for development of anticancer drugs Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
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

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Homo sapiens 5739
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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+ ?
-
?
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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
partially frim K-562 leukemic cells Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell liver carcinoma cell line Homo sapiens
-
K-562 cell leukemia cell line Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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+ Homo sapiens ?
-
?
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
Homo sapiens nicotinamide D-ribonucleotide + diphosphate
-
?
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide Homo sapiens nicotinamide D-ribonucleotide + diphosphate
-
?

Synonyms

Synonyms Comment Organism
NAPRT
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8.8
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0003
-
FK866 free enzyme Homo sapiens
0.0004
-
FK866 enzyme-substrate complex Homo sapiens