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Literature summary for 1.1.1.64 extracted from

  • Skarydova, L.; Hofman, J.; Chlebek, J.; Havrankova, J.; Kosanova, K.; Skarka, A.; Hostalkova, A.; Plucha, T.; Cahlikova, L.; Wsol, V.
    Isoquinoline alkaloids as a novel type of AKR1C3 inhibitors (2014), J. Steroid Biochem. Mol. Biol., 143, 250-258.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2'-hydroxyflavanone
-
Homo sapiens
canadine
-
Homo sapiens
corydaline
-
Homo sapiens
corypalmine
-
Homo sapiens
indomethacin
-
Homo sapiens
additional information nineteen isoquinoline alkaloids were examined for their ability to inhibit a recombinant AKR1C3 enzyme Homo sapiens
scoulerine
-
Homo sapiens
Stylopine the most potent inhibitor among the tested compounds that exhibited moderate selectivity towards AKR1C3 versus AKR1C1, EC 1.1.1.62. Stylopine significantly inhibits the AKR1C3-mediated reduction of daunorubicin in intact cells without considerable cytotoxic effects Homo sapiens
tetrahydrocolumbamine
-
Homo sapiens
tetrahydroplamatine
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
testosterone + NADP+ Homo sapiens
-
androstenedione + NADPH + H+
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens P42330
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adenocarcinoma cell
-
Homo sapiens
-
HCT-116 cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
additional information the enzyme is frequently upregulated in various cancers Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
17beta-estradiol + NADP+
-
Homo sapiens estrone + NADPH
-
r
testosterone + NADP+
-
Homo sapiens androstenedione + NADPH + H+
-
r

Synonyms

Synonyms Comment Organism
AKR1C3
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00046
-
pH 7.4, 37°C, determined with the oracin to dihydrooracin assay Homo sapiens indomethacin
0.0009
-
pH 7.4, 37°C, determined with the oracin to dihydrooracin assay Homo sapiens Stylopine
0.0037
-
pH 7.4, 37°C, determined with the reduction of androstenedione to testosterone assay Homo sapiens indomethacin
0.0077
-
pH 7.4, 37°C, determined with the reduction of androstenedione to testosterone assay Homo sapiens Stylopine
0.0122
-
pH 7.4, 37°C, determined with the oracin to dihydrooracin assay Homo sapiens canadine
0.029
-
pH 7.4, 37°C, determined with the reduction of androstenedione to testosterone assay Homo sapiens canadine

General Information

General Information Comment Organism
physiological function AKR1C3 is an important human enzyme that participates in the reduction of steroids and prostaglandins, which leads to proliferative signalling. In addition, this enzyme also participates in the biotransformation of xenobiotics, such as drugs and procarcinogens. AKR1C3 is involved in the development of both hormone-dependent and hormone-independent cancers and confers cell resistance to anthracyclines. Role ofAKR1C3in hormone-dependent (e.g., breast, prostate and endometrium) and hormone-independent (e.g., lung, brain, and kidney) cancers Homo sapiens