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 (Comment) | Organism |
---|---|
- |
Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P16152 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
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 | Comment | Organism |
---|---|---|
carbonyl reductase 1 | - |
Homo sapiens |
CBR1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
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 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 |