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Literature summary for 1.1.1.188 extracted from

  • Lovering, A.L.; Ride, J.P.; Bunce, C.M.; Desmond, J.C.; Cummings, S.M.; White, S.A.
    Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin (2004), Cancer Res., 64, 1802-1810.
    View publication on PubMed

Application

Application Comment Organism
pharmacology enzyme is a target for cyclooxygenase-independent antineoplastic actions of nonsteroidal anti-inflammatory drugs Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli BL21(DE3) Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
16 mg/ml purified enzyme complexed with inhibitors acetate, flufenamic acid or indomethacin, hanging drop vapour diffusion method in 0.006 ml drops, 1:1 mixture of protein solution containing 10 mM potassium phosphate, pH 7.0, 1 mM DTT, 1 mM EDTA, 2 mM NADP+, with reservoir solution containing 25% w/v PEG 4000, 100 mM sodium citrate, pH 6.0, 2.5% v/v 2-methyl-2,4-pentanediol, and 800 mM ammonium acetate, 6 days to maximum size, X-ray diffraction structure determination of the complexes and analysis at 1.2-2.1 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acetate occupies the oxyanion hole of the active site, 2 complex structures Homo sapiens
Flufenamic acid nonsteroidal anti-inflammatory drug, binds to both the active site and the beta-hairpin loop at the opposite end of the central beta-barrel, complex structure Homo sapiens
indomethacin nonsteroidal anti-inflammatory drug, 1 molecule binds to the active site, complex structure Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics of 3alpha-hydroxysteroid dehydrogenase type II activity Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42330
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme from Escherichia coli to homogeneity Homo sapiens

Reaction

Reaction Comment Organism Reaction ID
(5Z,13E)-(15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dienoate + NADP+ = (5Z,13E)-(15S)-9alpha,15-dihydroxy-11-oxoprosta-5,13-dienoate + NADPH + H+ active site structure, enzyme also shows 3alpha-hydroxysteroid dehydrogenase type II activity, i.e. 3alpha-HSD Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information acive site structure, enzyme also shows 3alpha-hydroxysteroid dehydrogenase type II activity Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
AKR1C3
-
Homo sapiens
More enzyme belongs to the aldo-keto reductase AKR family, enzyme also shows 3alpha-hydroxysteroid dehydrogenase type II activity, i.e. 3alpha-HSD Homo sapiens
PGFS
-
Homo sapiens
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
additional information
-
additional information Ki values for the nonsteroidal anti-inflammatory drug inhibitors with 3alpha-androstanediol as a substrate Homo sapiens