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Literature summary extracted from

  • Byrns, M.; Penning, T.
    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.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
1.1.1.188 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)

EC Number Cloned (Comment) Organism
1.1.1.188 overexpression of AKR1C3 using a pLNCX retroviral vector in MCF-7 cell line Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.188 AKR1C3 in complex with NADP+ and indomethacin Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.188 4-benzoyl-benzoic acid
-
 Homo sapiens
1.1.1.188 4-carboxy-2',4'-dinitrodiphenylamine
-
 Homo sapiens
1.1.1.188 4-carboxy-2-aminodiphenylamine
-
 Homo sapiens
1.1.1.188 4-chloro-N-(4-tolyl)-anthranilic acid
-
 Homo sapiens
1.1.1.188 4-chloro-N-phenylanthranilic acid
-
 Homo sapiens
1.1.1.188 4-nitro-N-phenylanthranilic acid
-
 Homo sapiens
1.1.1.188 5-methyl-N-phenylanthranilic acid
-
 Homo sapiens
1.1.1.188 aspirin
-
 Homo sapiens
1.1.1.188 flurbiprofen
-
 Homo sapiens
1.1.1.188 Ibuprofen
-
 Homo sapiens
1.1.1.188 indomethacin inhibits AKR1C3, but does not inhibit highly related AKR1C1 or AKR1C2 Homo sapiens
1.1.1.188 Meclofenamic acid
-
 Homo sapiens
1.1.1.188 Mefenamic acid
-
 Homo sapiens
1.1.1.188 additional information AKR1C3 is potently inhibited by non-steroidal anti-inflammatory drugs, which are protective against breast cancer Homo sapiens
1.1.1.188 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
1.1.1.188 naproxen
-
 Homo sapiens
1.1.1.188 salicylic acid
-
 Homo sapiens
1.1.1.188 sulindac
-
 Homo sapiens
1.1.1.188 Zomepirac
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.188 Homo sapiens
-
-
-
1.1.1.188 Homo sapiens P42330
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.188 breast normal breast expresses very high levels of AKR1C3 relative to other tissues Homo sapiens
-
1.1.1.188 breast cancer cell 18fold increase in the median AKR1C3 mRNA levels in breast cancer patients as compared to those without disease Homo sapiens
-
1.1.1.188 MCF-7 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.188 9,10-phenanthrenequinone + NADPH + H+
-
 Homo sapiens ?
-
 ?
1.1.1.188 prostaglandin D2 + NADPH + H+
-
 Homo sapiens 9alpha,11beta-prostaglandin F2 + NADP+
-
 ?
1.1.1.188 prostaglandin H2 + NADPH + H+
-
 Homo sapiens prostaglandin F2alpha + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.188 AKR1C3
-
 Homo sapiens
1.1.1.188 aldo-keto reductase 1C3
-
 Homo sapiens
1.1.1.188 type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.188 NADPH
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.188 0.0003
-
 Mefenamic acid
-
 Homo sapiens
1.1.1.188 0.00038
-
 4-carboxy-2',4'-dinitrodiphenylamine
-
 Homo sapiens
1.1.1.188 0.0014
-
 4-chloro-N-(4-tolyl)-anthranilic acid
-
 Homo sapiens
1.1.1.188 0.0019
-
 4-nitro-N-phenylanthranilic acid
-
 Homo sapiens
1.1.1.188 0.0019
-
 4-benzoyl-benzoic acid
-
 Homo sapiens
1.1.1.188 0.0029
-
 4-chloro-N-phenylanthranilic acid
-
 Homo sapiens
1.1.1.188 0.0034
-
 N-(4-chlorobenzoyl)-melatonin
-
 Homo sapiens
1.1.1.188 0.0073
-
 5-methyl-N-phenylanthranilic acid
-
 Homo sapiens
1.1.1.188 0.01
-
 4-carboxy-2-aminodiphenylamine
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.188 0.00039
-
-
 Homo sapiens Mefenamic acid
1.1.1.188 0.0004
-
-
 Homo sapiens 4-carboxy-2',4'-dinitrodiphenylamine
1.1.1.188 0.0007
-
-
 Homo sapiens Meclofenamic acid
1.1.1.188 0.0014
-
-
 Homo sapiens naproxen
1.1.1.188 0.0015
-
-
 Homo sapiens 4-chloro-N-(4-tolyl)-anthranilic acid
1.1.1.188 0.002
-
-
 Homo sapiens 4-nitro-N-phenylanthranilic acid
1.1.1.188 0.002
-
-
 Homo sapiens 4-benzoyl-benzoic acid
1.1.1.188 0.0023
-
-
 Homo sapiens indomethacin
1.1.1.188 0.003
-
-
 Homo sapiens 4-chloro-N-phenylanthranilic acid
1.1.1.188 0.0034
-
-
 Homo sapiens sulindac
1.1.1.188 0.0078
-
-
 Homo sapiens flurbiprofen
1.1.1.188 0.0099
-
-
 Homo sapiens Ibuprofen
1.1.1.188 0.011
-
-
 Homo sapiens 5-methyl-N-phenylanthranilic acid
1.1.1.188 0.011
-
-
 Homo sapiens 4-carboxy-2-aminodiphenylamine
1.1.1.188 0.04
-
-
 Homo sapiens Zomepirac
1.1.1.188 0.77
-
-
 Homo sapiens salicylic acid
1.1.1.188 1.2
-
-
 Homo sapiens aspirin