Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
5-methoxy-1,2-dimethyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione | ES936, potent inhibitor of NQO1 activity and cell proliferation. Approximately 90% inhibition of enzyme activity after 4 h. Inactivation is dependent upon NADH | Homo sapiens | |
5-methoxy-1,2-dimethyl-3-[(4-pyridinyloxy)methyl]indole-4,7-dione | approximately 90% inhibition of enzyme activity after 4 h, and this inactivation is dependent upon NADH | Homo sapiens | |
6-methoxy-1,2-dimethyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione | approximately 90% inhibition of enzyme activity after 4 h, and this inactivation is dependent upon NADH | Homo sapiens | |
6-methoxy-1,2-dimethyl-3-[(4-pyridinyloxy)methyl]indole-4,7-dione | approximately 90% inhibition of enzyme activity after 4 h, and this inactivation is dependent upon NADH | Homo sapiens | |
6-methoxy-1,2-dimethyl-3-[(acetoxy)methyl]indole-4,7-dione | approximately 90% inhibition of enzyme activity after 4 h, and this inactivation is dependent upon NADH | Homo sapiens | |
additional information | indolequinones with 4-nitrophenoxy, 4-pyridinyloxy, and acetoxy substituents at the (indol-3-yl)methyl position are NADH-dependent inhibitors of recombinant human NQO1, indicative of mechanism-based inhibition. However, those with hydroxy and phenoxy substituents are poor inhibitors of NQO1 enzyme activity, due to attenuated elimination of the leaving group. 4-pyridinyloxy and acetoxy compounds are potent inhibitors of NQO1 activity but relatively poor inhibitors of cell proliferation. Phenoxy compounds, which are not inhibitors of NQO1 enzymatic activity, demonstrate potent growth inhibition | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P15559 | - |
- |
Purification (Comment) | Organism |
---|---|
by affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
MiaPaCa-2 cell | - |
Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
800 | - |
purified enzyme | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
5-methoxy-1,2-dimethyl-3-(hydroxymethyl)indole-4,7-dione + NADH | is efficiently metabolized by NQO1 | Homo sapiens | ? + NAD+ | - |
? | |
5-methoxy-1,2-dimethyl-3-[(phenoxy)methyl]indole-4,7-dione + NADH | inefficient indolequinone substrate | Homo sapiens | ? + NAD+ | - |
? | |
6-methoxy-1,2-dimethyl-3-(hydroxymethyl)indole-4,7-dione + NADH | is efficiently metabolized by NQO1 | Homo sapiens | ? + NAD+ | - |
? | |
6-methoxy-1,2-dimethyl-3-[(phenoxy)methyl]indole-4,7-dione + NADH | inefficient indolequinone substrate | Homo sapiens | ? + NAD+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
DT-diaphorase | - |
Homo sapiens |
EC 1.6.99.2 | formerly | Homo sapiens |
NAD(P)H:quinone oxidoreductase 1 | - |
Homo sapiens |
NQO1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | - |
Homo sapiens |