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Literature summary for 1.1.1.188 extracted from
- Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3): Role in breast cancer and inhibition by non-steroidal anti-inflammatory drug analogs (2009), Chem. Biol. Interact., 178, 221-227.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | AKR1C3 likely plays important roles in the development of hormone-dependent, and possibly hormone-independent, breast cancer. It is highly expressed in normal breast and upregulated in breast cancer, where its expression is associated with a worse prognosis | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| overexpression of AKR1C3 using a pLNCX retroviral vector in MCF-7 cell line | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| AKR1C3 in complex with NADP+ and indomethacin | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-benzoyl-benzoic acid | - |
Homo sapiens |  |
| 4-carboxy-2',4'-dinitrodiphenylamine | - |
Homo sapiens | |
| 4-carboxy-2-aminodiphenylamine | - |
Homo sapiens | |
| 4-chloro-N-(4-tolyl)-anthranilic acid | - |
Homo sapiens | |
| 4-chloro-N-phenylanthranilic acid | - |
Homo sapiens | |
| 4-nitro-N-phenylanthranilic acid | - |
Homo sapiens | |
| 5-methyl-N-phenylanthranilic acid | - |
Homo sapiens | |
| aspirin | - |
Homo sapiens | |
| flurbiprofen | - |
Homo sapiens | |
| Ibuprofen | - |
Homo sapiens | |
| indomethacin | inhibits AKR1C3, but does not inhibit highly related AKR1C1 or AKR1C2 | Homo sapiens | |
| Meclofenamic acid | - |
Homo sapiens | |
| Mefenamic acid | - |
Homo sapiens | |
| additional information | AKR1C3 is potently inhibited by non-steroidal anti-inflammatory drugs, which are protective against breast cancer | Homo sapiens | |
| N-(4-chlorobenzoyl)-melatonin | exhibits uncompetitive inhibition patterns for the reduction of 9,10-phenanthrenequinone but competitive inhibition patterns for the reduction of androstenedione by AKR1C3 | Homo sapiens | |
| naproxen | - |
Homo sapiens | |
| salicylic acid | - |
Homo sapiens | |
| sulindac | - |
Homo sapiens | |
| Zomepirac | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Homo sapiens | P42330 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| breast | normal breast expresses very high levels of AKR1C3 relative to other tissues | Homo sapiens | - |
| breast cancer cell | 18fold increase in the median AKR1C3 mRNA levels in breast cancer patients as compared to those without disease | Homo sapiens | - |
| MCF-7 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 9,10-phenanthrenequinone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| prostaglandin D2 + NADPH + H+ | - |
Homo sapiens | 9alpha,11beta-prostaglandin F2 + NADP+ | - |
? | |
| prostaglandin H2 + NADPH + H+ | - |
Homo sapiens | prostaglandin F2alpha + NADP+ | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AKR1C3 | - |
Homo sapiens |
| aldo-keto reductase 1C3 | - |
Homo sapiens |
| type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADPH | - |
Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0003 | - |
Mefenamic acid | - |
Homo sapiens | |
| 0.00038 | - |
4-carboxy-2',4'-dinitrodiphenylamine | - |
Homo sapiens | |
| 0.0014 | - |
4-chloro-N-(4-tolyl)-anthranilic acid | - |
Homo sapiens | |
| 0.0019 | - |
4-nitro-N-phenylanthranilic acid | - |
Homo sapiens | |
| 0.0019 | - |
4-benzoyl-benzoic acid | - |
Homo sapiens | |
| 0.0029 | - |
4-chloro-N-phenylanthranilic acid | - |
Homo sapiens | |
| 0.0034 | - |
N-(4-chlorobenzoyl)-melatonin | - |
Homo sapiens | |
| 0.0073 | - |
5-methyl-N-phenylanthranilic acid | - |
Homo sapiens | |
| 0.01 | - |
4-carboxy-2-aminodiphenylamine | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00039 | - |
- |
Homo sapiens | Mefenamic acid | |
| 0.0004 | - |
- |
Homo sapiens | 4-carboxy-2',4'-dinitrodiphenylamine | |
| 0.0007 | - |
- |
Homo sapiens | Meclofenamic acid | |
| 0.0014 | - |
- |
Homo sapiens | naproxen | |
| 0.0015 | - |
- |
Homo sapiens | 4-chloro-N-(4-tolyl)-anthranilic acid | |
| 0.002 | - |
- |
Homo sapiens | 4-nitro-N-phenylanthranilic acid | |
| 0.002 | - |
- |
Homo sapiens | 4-benzoyl-benzoic acid | |
| 0.0023 | - |
- |
Homo sapiens | indomethacin | |
| 0.003 | - |
- |
Homo sapiens | 4-chloro-N-phenylanthranilic acid | |
| 0.0034 | - |
- |
Homo sapiens | sulindac | |
| 0.0078 | - |
- |
Homo sapiens | flurbiprofen | |
| 0.0099 | - |
- |
Homo sapiens | Ibuprofen | |
| 0.011 | - |
- |
Homo sapiens | 5-methyl-N-phenylanthranilic acid | |
| 0.011 | - |
- |
Homo sapiens | 4-carboxy-2-aminodiphenylamine | |
| 0.04 | - |
- |
Homo sapiens | Zomepirac | |
| 0.77 | - |
- |
Homo sapiens | salicylic acid | |
| 1.2 | - |
- |
Homo sapiens | aspirin | |
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