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Literature summary for 1.1.1.62 extracted from

  • Bertoletti, N.; Braun, F.; Lepage, M.; Moeller, G.; Adamski, J.; Heine, A.; Klebe, G.; Marchais-Oberwinkler, S.
    New insights into human 17beta-hydroxysteroid dehydrogenase type 14: first crystal structures in complex with a steroidal ligand and with a potent nonsteroidal inhibitor (2016), J. Med. Chem., 59, 6961-6967.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of 17beta-HSD14 wild-type variants S205 and T205 in Escherichia coli strain BL21 pLysS Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
the purified enzyme variants T205 and S205 in apoform, as holoenzyme, or in complex with estrone or inhibitor [6-(3,4-dihydroxyphenyl)pyridin-2-yl]-(4-fluoro-3-hydroxyphenyl)methanone, ternary complex enzyme-cofactor-inhibitor, X-ray diffraction structure determination and analysis at 1.52-2.02 A resolution Homo sapiens

Protein Variants

Protein Variants Comment Organism
S205T natural genetic polymorphism Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
[6-(3,4-dihydroxyphenyl)pyridin-2-yl]-(4-fluoro-3-hydroxyphenyl)methanone a potent nonsteroidal inhibitor, binding structure, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information Michaelis-Menten kinetics Homo sapiens
0.00062
-
17beta-estradiol 17beta-HSD14 variant S205, pH and temperature not specified in the publication Homo sapiens
0.00079
-
17beta-estradiol 17beta-HSD14 variant T205, pH and temperature not specified in the publication Homo sapiens
0.0066
-
5-androstene-3beta,17beta-diol 17beta-HSD14 variant S205, pH and temperature not specified in the publication Homo sapiens
0.0078
-
5-androstene-3beta,17beta-diol 17beta-HSD14 variant T205, pH and temperature not specified in the publication Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
17beta-estradiol + NAD+ Homo sapiens
-
estrone + NADH + H+
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BPX1
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adrenal gland
-
Homo sapiens
-
brain
-
Homo sapiens
-
breast cancer cell
-
Homo sapiens
-
esophagus
-
Homo sapiens
-
eye
-
Homo sapiens
-
heart
-
Homo sapiens
-
kidney
-
Homo sapiens
-
liver
-
Homo sapiens
-
placenta
-
Homo sapiens
-
rectum
-
Homo sapiens
-
salivary gland
-
Homo sapiens
-
skeletal muscle
-
Homo sapiens
-
testis
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
17beta-estradiol + NAD+
-
Homo sapiens estrone + NADH + H+
-
r
5-androstene-3beta,17beta-diol + NAD+
-
Homo sapiens ? + NADH + H+
-
?
testosterone + NAD+
-
Homo sapiens androst-4-ene-3,17-dione + NADH + H+
-
?

Synonyms

Synonyms Comment Organism
17beta-HSD14
-
Homo sapiens
17beta-hydroxysteroid dehydrogenase type 14
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00028
-
5-androstene-3beta,17beta-diol 17beta-HSD14 variant S205, pH and temperature not specified in the publication Homo sapiens
0.00032
-
5-androstene-3beta,17beta-diol 17beta-HSD14 variant T205, pH and temperature not specified in the publication Homo sapiens
0.0004
-
17beta-estradiol 17beta-HSD14 variant S205, pH and temperature not specified in the publication Homo sapiens
0.00055
-
17beta-estradiol 17beta-HSD14 variant T205, pH and temperature not specified in the publication Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+
-
Homo sapiens
NADH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000007
-
[6-(3,4-dihydroxyphenyl)pyridin-2-yl]-(4-fluoro-3-hydroxyphenyl)methanone pH and temperature not specified in the publication Homo sapiens