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 | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
testosterone + NADP+ | Homo sapiens | - |
androstenedione + NADPH + H+ | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P42330 | - |
- |
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 | 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 | Comment | Organism |
---|---|---|
AKR1C3 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADP+ | - |
Homo sapiens | |
NADPH | - |
Homo sapiens |
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 | 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 |