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Literature summary for 1.1.1.62 extracted from

  • Frotscher, M.; Ziegler, E.; Marchais-Oberwinkler, S.; Kruchten, P.; Neugebauer, A.; Fetzer, L.; Scherer, C.; Mueller-Vieira, U.; Messinger, J.; Thole, H.; Hartmann, R.W.
    Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease (2008), J. Med. Chem., 51, 2158-2169.
    View publication on PubMed
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Application

Application Comment Organism
medicine 17beta-HSD1 is overexpressed in many breast tumors. Thus, it is an attractive target for the treatment of these diseases Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(3-hydroxyphenyl)quinolin-6-ol 0.001 mM, 63% inhibition, substrate: estrone Homo sapiens
3-(2-naphthyl)phenol 0.001 mM, 61% inhibition, substrate: estrone Homo sapiens
3-(3-hydroxyphenyl)quinolin-7-ol 0.001 mM, 57% inhibition, substrate: estrone Homo sapiens
3-(6-hydroxy-2-naphthyl)benzoic acid 0.001 mM, 76% inhibition, substrate: estrone Homo sapiens
3-(quinolin-3-yl)phenol 0.001 mM, 18% inhibition, substrate: estrone Homo sapiens
5-(6-hydroxy-2-naphthyl)pyridin-3-ol 0.001 mM, 58% inhibition, substrate: estrone Homo sapiens
6-(3-hydroxyphenyl)-1-naphthol 0.001 mM, 23% inhibition, substrate: estrone Homo sapiens
6-(3-hydroxyphenyl)-2-naphthol 0.0001 mM, 91% inhibition, substrate: estrone Homo sapiens
6-(3-hydroxyphenyl)-3,4-dihydronaphthalen-1(2H)-one 0.001 mM, 23% inhibition, substrate: estrone Homo sapiens
6-(4-hydroxyphenyl)-1-naphthol 0.001 mM, 55% inhibition, substrate: estrone Homo sapiens
6-pyridin-3-yl-2-naphthol 0.001 mM, 32% inhibition, substrate: estrone Homo sapiens
6-[4-(hydroxymethyl)phenyl]-2-naphthol 0.001 mM, 13% inhibition, substrate: estrone Homo sapiens
7-(3-hydroxyphenyl)-2-naphthol 0.001 mM, 62% inhibition, substrate: estrone Homo sapiens
N-[3-(6-hydroxy-2-naphthyl)phenyl]acetamide 0.001 mM, 19% inhibition, substrate: estrone Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell 17beta-HSD1 is overexpressed in many breast tumors Homo sapiens
-
placenta
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone + NADPH + H+
-
 Homo sapiens estradiol-17beta + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
17beta-HSD1
-
 Homo sapiens
17beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens