Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary 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

Crystallization (Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.188 1-(4-aminobenzyl)-5-methoxy-2-methylindoleacetic acid
-
 Homo sapiens
1.1.1.188 flurbiprofen
-
 Homo sapiens
1.1.1.188 Ibuprofen
-
 Homo sapiens
1.1.1.188 indomethacin specific inhibition of isoform AKR1C3 versus AKR1C1 and AKR1C3 Homo sapiens
1.1.1.188 indomethacin methyl ester specific inhibition of isoform AKR1C3 versus AKR1C1 and AKR1C3 Homo sapiens
1.1.1.188 Meclofenamic acid
-
 Homo sapiens
1.1.1.188 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
1.1.1.188 naproxen
-
 Homo sapiens
1.1.1.188 sulindac
-
 Homo sapiens
1.1.1.188 Zomepirac
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.188 0.0015
-
 9,10-phenanthrenequinone pH 7.0, 37°C Homo sapiens
1.1.1.188 0.0066
-
 androst-4-ene-3,17-dione pH 7.0, 37°C Homo sapiens

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.188 9,10-phenanthrenequinone + NADPH
-
 Homo sapiens ? + NADP+
-
 ?
1.1.1.188 androst-4-ene-3,17-dione + NADPH
-
 Homo sapiens ? + NADP+
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.1.1.188 0.0027
-
 androst-4-ene-3,17-dione pH 7.0, 37°C Homo sapiens
1.1.1.188 1.4
-
 9,10-phenanthrenequinone pH 7.0, 37°C Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.188 NADP+
-
 Homo sapiens
1.1.1.188 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.188 0.0007
-
 pH 7.0, 37°C Homo sapiens Meclofenamic acid
1.1.1.188 0.0014
-
 pH 7.0, 37°C Homo sapiens naproxen
1.1.1.188 0.0023
-
 pH 7.0, 37°C Homo sapiens indomethacin
1.1.1.188 0.0023
-
 pH 7.0, 37°C Homo sapiens indomethacin methyl ester
1.1.1.188 0.0034
-
 pH 7.0, 37°C Homo sapiens sulindac
1.1.1.188 0.0078
-
 pH 7.0, 37°C Homo sapiens flurbiprofen
1.1.1.188 0.0078
-
 pH 7.0, 37°C Homo sapiens N-(4-chlorobenzoyl)-melatonin
1.1.1.188 0.0099
-
 pH 7.0, 37°C Homo sapiens Ibuprofen
1.1.1.188 0.04
-
 pH 7.0, 37°C Homo sapiens Zomepirac
1.1.1.188 0.052
-
 pH 7.0, 37°C Homo sapiens 1-(4-aminobenzyl)-5-methoxy-2-methylindoleacetic acid