Crystallization (Comment) | Organism |
---|---|
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 | Comment | Organism | Structure |
---|---|---|---|
3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide | - |
Homo sapiens | |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
breast | - |
Homo sapiens | - |
breast cancer cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
estrone + NADPH + H+ | - |
Homo sapiens | estradiol-17beta + NADP+ | - |
? | |
testosterone + NADP+ | - |
Homo sapiens | 4-androstene-3,17-dione + NADPH + H+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
17beta-HSD1 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
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 | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
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 |
Organism | Comment | Expression |
---|---|---|
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 | Comment | Organism |
---|---|---|
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 |