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Literature summary for 1.1.1.184 extracted from

  • Kassner, N.; Huse, K.; Martin, H.J.; Goedtel-Armbrust, U.; Metzger, A.; Meineke, I.; Brockmoeller, J.; Klein, K.; Zanger, U.M.; Maser, E.; Wojnowski, L.
    Carbonyl reductase 1 is a predominant doxorubicin reductase in the human liver (2008), Drug Metab. Dispos., 36, 2113-2120.
    View publication on PubMed

Application

Application Comment Organism
drug development CBR1 inhibition can improve the therapeutic response to doxorubicin and reduce its side effects Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
CBR1 expressed as histidine-tagged protein Homo sapiens
CBR3 expressed as histidine-tagged protein Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-amino-1-tert-butyl-3-(2-hydroxyphenyl)pyrazolo[3,4-d]pyrimidine
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.132
-
doxorubicin in stomach Homo sapiens
0.134
-
doxorubicin in kidney Homo sapiens
0.14
-
doxorubicin in colon Homo sapiens
0.163
-
doxorubicin in liver Homo sapiens
0.167
-
doxorubicin purified enzyme Homo sapiens
0.231
-
doxorubicin in lung Homo sapiens
0.239
-
doxorubicin in heart Homo sapiens
0.244
-
doxorubicin in skeletal muscle Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P16152
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
colon
-
Homo sapiens
-
colon low expression of CBR3 Homo sapiens
-
heart
-
Homo sapiens
-
heart low expression of CBR3 Homo sapiens
-
kidney
-
Homo sapiens
-
kidney low expression of CBR3 Homo sapiens
-
liver CBR1 is prominently expressed in the liver Homo sapiens
-
liver low expression of CBR3 Homo sapiens
-
lung
-
Homo sapiens
-
lung low expression of CBR3 Homo sapiens
-
skeletal muscle
-
Homo sapiens
-
skeletal muscle low expression of CBR3 Homo sapiens
-
stomach
-
Homo sapiens
-
stomach low expression of CBR3 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
9,10-phenanthrenequinone + NADPH + H+
-
Homo sapiens ? + NADP+
-
?
doxorubicin + NADPH + H+ CBR1 is a predominant hepatic doxorubicin reductase Homo sapiens doxorubicinol + NADP+
-
?
menadione + NADPH + H+
-
Homo sapiens ? + NADP+
-
?
additional information no doxorubicin or menadione reduction is catalyzed by CBR3 Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
carbonyl reductase 1
-
Homo sapiens
CBR1
-
Homo sapiens
CBR3
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0103
-
doxorubicin
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0105
-
4-amino-1-tert-butyl-3-(2-hydroxyphenyl)pyrazolo[3,4-d]pyrimidine for doxorubicin metabolism Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0013
-
for menadione metabolism Homo sapiens 4-amino-1-tert-butyl-3-(2-hydroxyphenyl)pyrazolo[3,4-d]pyrimidine