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Literature summary for 1.1.1.62 extracted from

  • Bey, E.; Marchais-Oberwinkler, S.; Kruchten, P.; Frotscher, M.; Werth, R.; Oster, A.; Alguel, O.; Neugebauer, A.; Hartmann, R.W.
    Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases (2008), Bioorg. Med. Chem., 16, 6423-6435.
    View publication on PubMed

Application

Application Comment Organism
medicine 17beta-HSD1 is an attractive target for the treatment of mammary tumours Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol 17beta-HSD1; substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol 17beta-HSD1; substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol 17beta-HSD1 Homo sapiens
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol 17beta-HSD1; substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol substrate: estradiol-17beta, 17beta-HSD2, very good selectivity, high cell permeability and medium CaCo-2 permeability; very good selectivity, high cell permeability and medium CaCo-2 permeability, 17beta-HSD1 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol 17beta-HSD1 Homo sapiens 5829
-
microsome 17beta-HSD2 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens P14061
-
-

Source Tissue

Source Tissue Comment Organism Textmining
placenta 17beta-HSD1 Homo sapiens
-
placenta 17beta-HSD2 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estradiol-17beta + NAD+ 17beta-HSD2 Homo sapiens estrone + NADH + H+
-
?
estrone + NADH + H+ 17beta-HSD1 Homo sapiens estradiol-17beta + NAD+
-
?

Synonyms

Synonyms Comment Organism
17beta-HSD1
-
Homo sapiens
17beta-HSD2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00025
-
substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens 3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
0.00027
-
substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens 3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
0.00031
-
substrate: estrone, 17beta-HSD1 Homo sapiens 3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
0.00084
-
substrate: estrone, 17beta-HSD1 Homo sapiens 3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
0.00132
-
substrate: estrone, 17beta-HSD1 Homo sapiens 3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
0.00161
-
substrate: estrone, 17beta-HSD1 Homo sapiens 3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
0.00185
-
substrate: estrone, 17beta-HSD1 Homo sapiens 3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
0.00728
-
substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens 3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
0.00812
-
substrate: estradiol-17beta, 17beta-HSD2 Homo sapiens 3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
0.0175
-
substrate: estrone, 17beta-HSD2 Homo sapiens 3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol