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Literature summary for 1.1.1.184 extracted from

  • Gonzalez-Covarrubias, V.; Kalabus, J.L.; Blanco, J.G.
    Inhibition of polymorphic human carbonyl reductase 1 (CBR1) by the cardioprotectant flavonoid 7-monohydroxyethyl rutoside (monoHER) (2008), Pharm. Res., 25, 1730-1734.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development the cardioprotectant 7-monohydroxyethylrutoside inhibits CBR1 activity. CBR1 V88I genotype status and the type of anthracycline substrate dictate the inhibition of CBR1 activity. Inhibition of CBR1 activity shall be considered during the development of novel cardioprotectants against anthracycline-related cardiotoxicity Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3',4',7-tris[O-(2-hydroxyethyl)]rutin
-
Homo sapiens
7-monohydroxyethylrutoside inhibits the activity of CBR1 V88 and CBR1 I88 in a concentration-dependent manner. It acts as a competitive CBR1 inhibitor when using daunorubicin as a substrate and acts as an uncompetitive CBR1 inhibitor for the small quinone substrate menadione. It inhibits the binding of NADPH in an uncompetitive manner for both substrates Homo sapiens
quercetin
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P16152
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
daunorubicin + NADPH + H+
-
Homo sapiens daunorubicinol + NADP+
-
?
doxorubicin + NADPH + H+
-
Homo sapiens doxorubicinol + NADP+
-
?
menadione + NADPH + H+
-
Homo sapiens ? + NADP+
-
?

Synonyms

Synonyms Comment Organism
carbonyl reductase 1
-
Homo sapiens
CBR1
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.033
-
7-monohydroxyethylrutoside CBR1 V88 with menadione as substrate Homo sapiens
0.045
-
7-monohydroxyethylrutoside CBR1 V88 with daunorubicin as substrate Homo sapiens
0.05
-
7-monohydroxyethylrutoside CBR1 V88 with cofactor NADPH, with a fixed 0.4 mM daunorubicin concentration Homo sapiens
0.14
-
7-monohydroxyethylrutoside CBR1 V88 with cofactor NADPH, with a fixed 0.15 mM menadione concentration Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.014
-
CBR1 I88 with daunorubicin as substrate Homo sapiens quercetin
0.019
-
CBR1 I88 with doxorubicin as substrate Homo sapiens quercetin
0.025
-
CBR1 V88 with daunorubicin as substrate Homo sapiens quercetin
0.034
-
CBR1 I88 with ddoxorubicin as substrate Homo sapiens 3',4',7-tris[O-(2-hydroxyethyl)]rutin
0.037
-
CBR1 I88 with doxorubicin as substrate Homo sapiens 7-monohydroxyethylrutoside
0.043
-
CBR1 V88 with doxorubicin as substrate Homo sapiens quercetin
0.053
-
CBR1 V88 with doxorubicin as substrate Homo sapiens 3',4',7-tris[O-(2-hydroxyethyl)]rutin
0.059
-
CBR1 V88 with doxorubicin as substrate Homo sapiens 7-monohydroxyethylrutoside
0.164
-
CBR1 I88 with daunorubicin as substrate Homo sapiens 7-monohydroxyethylrutoside
0.214
-
CBR1 I88 with daunorubicin as substrate Homo sapiens 3',4',7-tris[O-(2-hydroxyethyl)]rutin
0.219
-
CBR1 V88 with daunorubicin as substrate Homo sapiens 7-monohydroxyethylrutoside
0.383
-
CBR1 V88 with daunorubicin as substrate Homo sapiens 3',4',7-tris[O-(2-hydroxyethyl)]rutin