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Literature summary extracted from

  • Hong, Y.; Chen, S.
    Aromatase, estrone sulfatase, and 17beta-hydroxysteroid dehydrogenase: Structure-function studies and inhibitor development (2011), Mol. Cell. Endocrinol., 340, 120-126.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.62 crystal structure of 17beta-HSD1 complexed with testosterone or estradiol are shown. Both testosterone and estradiol bind in the narrow hydrophobic tunnel of 17beta-HSD1 with a high degree of complementarity. Testosterone is bound in an alternative orientation to 17beta-HSD1 compared with estradiol. Residue L149 plays an important role in the discrimination between C19 androgen and C18 estrogen Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.62 3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide
-
 Homo sapiens
1.1.1.62 9-(5-O-(9-[(16alpha,17alpha)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl)-alpha-L-arabinofuranosyl)-9H-purin-6-amine shows key interactions with two different enzyme-binding sites, namely the substrate- and the cofactor-binding sites Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.62 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.62 breast
-
 Homo sapiens
-
1.1.1.62 breast cancer cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.62 estrone + NADPH + H+
-
 Homo sapiens estradiol-17beta + NADP+
-
 ?
1.1.1.62 testosterone + NADP+
-
 Homo sapiens 4-androstene-3,17-dione + NADPH + H+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.62 17beta-HSD1
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.62 0.0000009
-
 3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide pH and temperature not specified in the publication Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.62 0.000042
-
 pH and temperature not specified in the publication Homo sapiens 3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide

Expression

EC Number Organism Comment Expression
1.1.1.62 Homo sapiens higher expression of 17beta-HSD1 mRNA is demonstrated in almost 50% of breast cancer tissues. Expression and activity of 17beta-HSD1 are significantly higher in breast cancer than in normal breast tissue up

General Information

EC Number General Information Comment Organism
1.1.1.62 physiological function enzyme involved in maintaining high estradiol levels in breast tumors of postmenopausal women. In certain breast cancer patients, intratumoral estradiol is produced by the 17beta-HSD1-mediated reduction of estrone produced by aromatase. A high level of 17-beta-HSD1 correlates with an increased risk of developing a late relapse of breast cancer in ER-positive breast cancer patients Homo sapiens