Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli strain BL21(DE3) | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
purified recombinant enzyme, hanging-drop, vapor-diffusion method, mixing of 0.001 ml of 4 mg/ml protein solution with 0.001 ml of reservoir solution containing 1.3-1.7 M ammonium sulfate, 0.1 M Bis-Tris buffer, pH 6.0-7.0, 0.1 M NaCl, 5 mM DTT, 0.012 mM FAD, and resveratrol, complexed with different inhibitors, X-ray diffraction structure determination and analysis at resolutions of 1.40-1.63 A | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(E)-3-(3,5-dihydroxyphenyl)-2-(4-hydroxyphenyl)acrylaldehyde | - |
Homo sapiens | |
(E)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)prop-2-en-1-ol | - |
Homo sapiens | |
(Z)-3-(3,5-dihydroxyphenyl)-2-(4-hydroxyphenyl)-acrylamide | - |
Homo sapiens | |
(Z)-3-(3,5-dihydroxyphenyl)-2-(4-hydroxyphenyl)acrylonitrile | - |
Homo sapiens | |
(Z)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylaldehyde | - |
Homo sapiens | |
(Z)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile | - |
Homo sapiens | |
(Z)-5-(3-hydroxy-2-(4-hydroxyphenyl)prop-1-en-1-yl)benzene-1,3-diol | - |
Homo sapiens | |
1,1'-(1E)-but-1-ene-1,2-diylbis(3,5-dimethoxybenzene) | - |
Homo sapiens | |
1,2-dimethoxy-4-[(1E)-2-(4-methoxyphenyl)prop-1-en-1-yl]benzene | - |
Homo sapiens | |
1,2-dimethoxy-4-[(E)-2-(3-methoxyphenyl)ethenyl]benzene | - |
Homo sapiens | |
1,2-dimethoxy-4-{(1Z)-3,3,3-trifluoro-2-[3-(trifluoromethyl)phenyl]prop-1-en-1-yl}benzene | - |
Homo sapiens | |
1,3-dimethoxy-5-[(1E)-2-(4-methoxyphenyl)prop-1-en-1-yl]benzene | - |
Homo sapiens | |
1,3-dimethoxy-5-[(1Z)-3,3,3-trifluoro-1-(4-methoxyphenyl)prop-1-en-2-yl]benzene | - |
Homo sapiens | |
1,3-dimethoxy-5-[(E)-2-(4-methoxyphenyl)ethenyl]benzene | - |
Homo sapiens | |
1-[(E)-2-(4-fluorophenyl)ethenyl]-3,5-dimethoxybenzene | - |
Homo sapiens | |
2-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]naphthalene | - |
Homo sapiens | |
2-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]naphthalene | - |
Homo sapiens | |
4-[(1E)-1-(3,5-dimethoxyphenyl)prop-1-en-2-yl]-1,2-dimethoxybenzene | - |
Homo sapiens | |
4-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-N,N-dimethylaniline | - |
Homo sapiens | |
4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]-1,2-dimethoxybenzene | - |
Homo sapiens | |
4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]phenol | - |
Homo sapiens | |
4-[(E)-2-(3-fluorophenyl)ethenyl]benzene-1,2-diol | - |
Homo sapiens | |
4-[(E)-2-(4-hydroxyphenyl)ethenyl]benzene-1,2-diol | - |
Homo sapiens | |
4-[(E)-2-(4-methoxyphenyl)ethenyl]benzene-1,2-diol | - |
Homo sapiens | |
4-{(1E)-1-[4-(trifluoromethyl)phenyl]prop-1-en-2-yl}phenol | - |
Homo sapiens | |
4-{(E)-2-[3-(trifluoromethyl)phenyl]ethenyl}benzene-1,2-diol | - |
Homo sapiens | |
5-[(1E)-1-(4-hydroxyphenyl)prop-1-en-2-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[(1E)-2-(3,4-dimethoxyphenyl)prop-1-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[(1E)-2-(4-hydroxyphenyl)prop-1-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-[(1E)-2-(4-methoxyphenyl)prop-1-en-1-yl]benzene-1,3-diol | - |
Homo sapiens | |
5-{(1E)-1-[4-(dimethylamino)phenyl]but-1-en-2-yl}benzene-1,3-diol | - |
Homo sapiens | |
additional information | enzyme inhibitor design, synthesiis, and evaluation, inhibitory potencies of resveratrol analogues, overview. Inhibitor binding structure, modelling, overview | Homo sapiens | |
N-(3,5-dihydroxyphenyl)-4-hydroxybenzamide | - |
Homo sapiens | |
resveratrol | i.e. 3,5,4'-trihydroxylstilbene, resveratrol binds tightly to the oxidized, FAD-form of the enzyme, and it acts as a competitive inhibitor against N-methyldihydronicotinamide. The amount of resveratrol consumed from dietary sources may be sufficient for effective inhibition of QR2 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | steady-state kinetic, overview | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant enzyme from Escherichia coli strain BL21(DE3) | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-methyldihydronicotinamide + 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide | - |
Homo sapiens | N-methylnicotinamide + ? | - |
? | |
N-methyldihydronicotinamide + menadione | - |
Homo sapiens | N-methylnicotinamide + menadiol | - |
? |
Synonyms | Comment | Organism |
---|---|---|
QR2 | - |
Homo sapiens |
quinone reductase 2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000088 | - |
resveratrol | versus N-methyldihydronicotinamide, pH and temperature not specified in the publication | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
physiological function | the enzyme functions in metabolic reduction and detoxification processes. Evidence exists linking QR2 to the metabolic activation of quinones, which can lead to cell toxicity. Inhibition of the enzymme by resveratrol may protect cells against reactive intermediates and eventually cancer | Homo sapiens |