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Literature summary for 1.1.1.149 extracted from

  • Matsunaga, T.; Yamaguchi, A.; Morikawa, Y.; Kezuka, C.; Takazawa, H.; Endo, S.; El-Kabbani, O.; Tajima, K.; Ikari, A.; Hara, A.
    Induction of aldo-keto reductases (AKR1C1 and AKR1C3) abolishes the efficacy of daunorubicin chemotherapy for leukemic U937 cells (2014), Anticancer Drugs, 25, 868-877.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene AKR1C1, real-time PCR expression anaysis Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
daunorubicin + NADPH + H+ Homo sapiens inactivation of the anticancer drug daunorubicinol + NADP+
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04828
-
-

Source Tissue

Source Tissue Comment Organism Textmining
colon carcinoma cell
-
Homo sapiens
-
additional information the expression of AKR1C1 is elevated in lung, uterine cervix, and colon cancers Homo sapiens
-
U-937 cell
-
Homo sapiens
-
uterine cervix carcinoma cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
daunorubicin + NADPH + H+ inactivation of the anticancer drug Homo sapiens daunorubicinol + NADP+
-
r
daunorubicin + NADPH + H+ the enzyme reduces daunorubicin to its corresponding alcohol daunorubicinol using NADPH as the coenzyme Homo sapiens daunorubicinol + NADP+
-
r

Synonyms

Synonyms Comment Organism
AKR1C1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens
NADPH
-
Homo sapiens

Expression

Organism Comment Expression
Homo sapiens the enzyme expression is upregulated by daunorubicin treament up

General Information

General Information Comment Organism
evolution the enzyme is a member of the aldo-keto reductase (AKR) superfamily that metabolizes endogenous substrates, such as carbohydrates, prostaglandins and steroids, and xenobiotics in a NAD(P)(H)-dependent manner Homo sapiens
physiological function crucial role of AKR1C1 in the acquisition of daunorubicin resistance of leukemic cells by metabolizing both daunorubicin and cytotoxic aldehydes derived from ROS-linked lipid peroxidation. Daunorubicin, at its sublethal doses, induces the expression of AKR1C1 and AKR1C3, EC 1.1.1.239, both of which reduce the daunorubicin sensitivity of the cells, AKR1C3 is more inducible than AKR1C1 by the daunorubicin treatment Homo sapiens