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Literature summary for 1.1.1.51 extracted from

  • Nashev, L.G.; Schuster, D.; Laggner, C.; Sodha, S.; Langer, T.; Wolber, G.; Odermatt, A.
    The UV-filter benzophenone-1 inhibits 17beta-hydroxysteroid dehydrogenase type 3: Virtual screening as a strategy to identify potential endocrine disrupting chemicals (2010), Biochem. Pharmacol., 79, 1189-1199.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293 cells by transient transfection Mus musculus
expressed in HEK-293 cells by transient transfection Rattus norvegicus
expressed in HEK-293 cells by transient transfection Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2,4-dihydroxyphenyl)-phenylmethanone remaining 17beta HSD3 activity: 1.1% Homo sapiens
(2,4-dihydroxyphenyl)-phenylmethanone (2,4-dihydroxyphenyl)-phenylmethanone leads to inhibition of testosterone synthesis in freshly isolated mouse and rat testis tissue Mus musculus
(2,4-dihydroxyphenyl)-phenylmethanone (2,4-dihydroxyphenyl)-phenylmethanone leads to inhibition of testosterone synthesis in freshly isolated mouse and rat testis tissue Rattus norvegicus
12-acetyl-11,12-dihydro-2-(trifluoromethyl)-6H-dibenzo(b,f)(1,4)thiazocine
-
Homo sapiens
12-acetyl-11,12-dihydro-6H-dibenzo(b,f)(1,4)thiazocine
-
Homo sapiens
2,2',4,4'-tetrahydroxybenzophenone remaining 17beta HSD3 activity: 47% Homo sapiens
2,5-dioxo-3-(2-propyn-1-yl)-3-pyrrolidinecarboxylic acid 2,3,3-triphenyl-2-propen-1-yl-ester
-
Homo sapiens
2-((3-chloro-4-hydroxybenzoyl)amino)-N-(2-(2-methoxyphenyl)ethyl)-5-phenoxy-benzamide
-
Homo sapiens
2-(5-acetyl-2-chloro-5,6,11,12-tetrahydrodibenzo(b,f)azocin-8-yl)-benzoic acid methyl ester
-
Homo sapiens
3-benzylidene camphor remaining 17beta HSD3 activity: 56% Homo sapiens
3alpha-butyl-3-hydroxy-5alpha-androstan-17-one
-
Homo sapiens
4-methylbenzylidene camphor remaining 17beta HSD3 activity: 33% Homo sapiens
5-acetyl-2-chloro-5,6-dihydro-dibenzo(b,f)azocine
-
Homo sapiens
5-acetyl-5,6,11,12-tetrahydro-dibenzo(b,f)(1,4)diazocine
-
Homo sapiens
androsterone
-
Homo sapiens
N-(((3,5)-3-hydroxy-17-oxoandrostan-3-yl)methyl)-N-(tricyclo(3.3.1.13.7)dec-2-ylmethyl)butanamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P37058
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
Mus musculus
-
testis
-
Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
17beta-HSD3
-
Mus musculus
17beta-HSD3
-
Rattus norvegicus
17beta-HSD3
-
Homo sapiens
17beta-hydroxysteroid dehydrogenase type 3
-
Mus musculus
17beta-hydroxysteroid dehydrogenase type 3
-
Rattus norvegicus
17beta-hydroxysteroid dehydrogenase type 3
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Mus musculus
37
-
assay at Rattus norvegicus
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Mus musculus
7.4
-
assay at Rattus norvegicus
7.4
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000002
-
pH and temperature not specified in the publication Homo sapiens 2-(5-acetyl-2-chloro-5,6,11,12-tetrahydrodibenzo(b,f)azocin-8-yl)-benzoic acid methyl ester
0.000035
-
pH and temperature not specified in the publication Homo sapiens N-(((3,5)-3-hydroxy-17-oxoandrostan-3-yl)methyl)-N-(tricyclo(3.3.1.13.7)dec-2-ylmethyl)butanamide
0.00006
-
pH and temperature not specified in the publication Homo sapiens 2-((3-chloro-4-hydroxybenzoyl)amino)-N-(2-(2-methoxyphenyl)ethyl)-5-phenoxy-benzamide
0.000116
-
pH and temperature not specified in the publication Homo sapiens 3alpha-butyl-3-hydroxy-5alpha-androstan-17-one
0.000182
-
pH and temperature not specified in the publication Homo sapiens androsterone
0.00024
-
pH and temperature not specified in the publication Homo sapiens 5-acetyl-2-chloro-5,6-dihydro-dibenzo(b,f)azocine
0.0004
-
pH and temperature not specified in the publication Homo sapiens 12-acetyl-11,12-dihydro-6H-dibenzo(b,f)(1,4)thiazocine
0.001
-
pH 7.4, 37°C Homo sapiens (2,4-dihydroxyphenyl)-phenylmethanone
0.00281
-
pH and temperature not specified in the publication Homo sapiens 12-acetyl-11,12-dihydro-2-(trifluoromethyl)-6H-dibenzo(b,f)(1,4)thiazocine
0.00474
-
pH and temperature not specified in the publication Homo sapiens 5-acetyl-5,6,11,12-tetrahydro-dibenzo(b,f)(1,4)diazocine
0.00915
-
pH and temperature not specified in the publication Homo sapiens 2,5-dioxo-3-(2-propyn-1-yl)-3-pyrrolidinecarboxylic acid 2,3,3-triphenyl-2-propen-1-yl-ester
0.0107
-
pH 7.4, 37°C Homo sapiens 4-methylbenzylidene camphor
0.0181
-
pH 7.4, 37°C Homo sapiens 2,2',4,4'-tetrahydroxybenzophenone
0.033
-
pH 7.4, 37°C Homo sapiens 3-benzylidene camphor