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Literature summary for 1.1.1.188 extracted from

  • Byrns, M.C.; Steckelbroeck, S.; Penning, T.M.
    An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies (2008), Biochem. Pharmacol., 75, 484-493.
    View publication on PubMedView publication on EuropePMC
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Crystallization (Commentary)

Crystallization (Comment) Organism
homology modeling of enzyme in complex with inhibitor indomethacin Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(4-aminobenzyl)-5-methoxy-2-methylindoleacetic acid
-
 Homo sapiens
flurbiprofen
-
 Homo sapiens
Ibuprofen
-
 Homo sapiens
indomethacin specific inhibition of isoform AKR1C3 versus AKR1C1 and AKR1C3 Homo sapiens
indomethacin methyl ester specific inhibition of isoform AKR1C3 versus AKR1C1 and AKR1C3 Homo sapiens
Meclofenamic acid
-
 Homo sapiens
N-(4-chlorobenzoyl)-melatonin specific inhibition of isoform AKR1C3 versus AKR1C1 and AKR1C3, not inhibitory to cyclooxygenases. Uncompetitive versus 9,10-phenynthrenequinone, competitive versus DELTA4-andostene-3,17-dione Homo sapiens
naproxen
-
 Homo sapiens
sulindac
-
 Homo sapiens
Zomepirac
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0015
-
 9,10-phenanthrenequinone pH 7.0, 37°C Homo sapiens
0.0066
-
 androst-4-ene-3,17-dione pH 7.0, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42330
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
9,10-phenanthrenequinone + NADPH
-
 Homo sapiens ? + NADP+
-
 ?
androst-4-ene-3,17-dione + NADPH
-
 Homo sapiens ? + NADP+
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0027
-
 androst-4-ene-3,17-dione pH 7.0, 37°C Homo sapiens
1.4
-
 9,10-phenanthrenequinone pH 7.0, 37°C Homo sapiens

Cofactor

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0007
-
 pH 7.0, 37°C Homo sapiens Meclofenamic acid
0.0014
-
 pH 7.0, 37°C Homo sapiens naproxen
0.0023
-
 pH 7.0, 37°C Homo sapiens indomethacin
0.0023
-
 pH 7.0, 37°C Homo sapiens indomethacin methyl ester
0.0034
-
 pH 7.0, 37°C Homo sapiens sulindac
0.0078
-
 pH 7.0, 37°C Homo sapiens flurbiprofen
0.0078
-
 pH 7.0, 37°C Homo sapiens N-(4-chlorobenzoyl)-melatonin
0.0099
-
 pH 7.0, 37°C Homo sapiens Ibuprofen
0.04
-
 pH 7.0, 37°C Homo sapiens Zomepirac
0.052
-
 pH 7.0, 37°C Homo sapiens 1-(4-aminobenzyl)-5-methoxy-2-methylindoleacetic acid