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Literature summary extracted from

  • Carlquist, M.; Frejd, T.; Gorwa-Grauslund, M.F.
    Flavonoids as inhibitors of human carbonyl reductase 1 (2008), Chem. Biol. Interact., 174, 98-108.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.184 expression in Sacchaormyces cerevisiae Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.184 computational docking experiments for four inhibitors. For flavonoid inhibitors, the flavonoid skeleton is the binding part of the molecule and sugar moieties are pointing outward, giving rise to a stabilizing effect Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.184 (2E)-1-(2,4-dihydroxyphenyl)-3-(2',4',6-trihydroxy-5'-[(2E)-3-(4-hydroxyphenyl)prop-2-enoyl]biphenyl-3-yl)prop-2-en-1-one
-
 Homo sapiens
1.1.1.184 3-(2-(2,4-dihydroxyphenyl)-1-[hydroxy(4-hydroxyphenyl)methyl]-2-oxoethyl)-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
-
 Homo sapiens
1.1.1.184 3-[2,3-dihydroxy-4-methoxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-4H-chromen-4-one
-
 Homo sapiens
1.1.1.184 3-[2-(2,4-dihydroxyphenyl)-1-(4-hydroxybenzyl)-2-oxoethyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
-
 Homo sapiens
1.1.1.184 7-O-beta-D-glucopyranos2-ulosyl-quercetin
-
 Homo sapiens
1.1.1.184 quercetin
-
 Homo sapiens
1.1.1.184 quercitrin
-
 Homo sapiens
1.1.1.184 rutin
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.184 0.0852
-
 daunorubicin pH 7.4, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.184 Homo sapiens P16152 isoform CBR1
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.184 recombinant protein Homo sapiens

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.1.1.184 161.6
-
 substrate daunorubicin, pH 7.4, 37°C Homo sapiens
1.1.1.184 1533
-
 substrate 2,3-butanedione, pH 7.4, 37°C Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.184 2,3-butanedione + NADPH
-
 Homo sapiens ? + NADP+
-
 ?
1.1.1.184 2-hydroxy-3-butanone + NADPH
-
 Homo sapiens 2,3-dihydroxybutanol + NADP+
-
 ?
1.1.1.184 daunorubicin + NADPH
-
 Homo sapiens daunorubicinol + NADP+
-
 ?
1.1.1.184 doxorubicin + NADPH
-
 Homo sapiens doxorubicinol + NADP+
-
 ?
1.1.1.184 ethyl acetoacetate + NADPH
-
 Homo sapiens ? + NADP+
-
 ?
1.1.1.184 menadione + NADPH
-
 Homo sapiens ? + NADP+
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.184 0.0011
-
 pH 7.4, 37°C Homo sapiens 3-[2-(2,4-dihydroxyphenyl)-1-(4-hydroxybenzyl)-2-oxoethyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
1.1.1.184 0.0021
-
 pH 7.4, 37°C Homo sapiens rutin
1.1.1.184 0.0036
-
 pH 7.4, 37°C Homo sapiens 3-(2-(2,4-dihydroxyphenyl)-1-[hydroxy(4-hydroxyphenyl)methyl]-2-oxoethyl)-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
1.1.1.184 0.0042
-
 pH 7.4, 37°C Homo sapiens (2E)-1-(2,4-dihydroxyphenyl)-3-(2',4',6-trihydroxy-5'-[(2E)-3-(4-hydroxyphenyl)prop-2-enoyl]biphenyl-3-yl)prop-2-en-1-one
1.1.1.184 0.0061
-
 pH 7.4, 37°C Homo sapiens 3-[2,3-dihydroxy-4-methoxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-4H-chromen-4-one
1.1.1.184 0.0062
-
 pH 7.4, 37°C Homo sapiens quercetin
1.1.1.184 0.0065
-
 pH 7.4, 37°C Homo sapiens quercitrin
1.1.1.184 0.008
-
 pH 7.4, 37°C Homo sapiens 7-O-beta-D-glucopyranos2-ulosyl-quercetin