Literature summary for 1.1.1.62 extracted from

Boutin, S.; Roy, J.; Maltais, R.; Alata, W.; Calon, F.; Poirier, D.
Identification of steroidal derivatives inhibiting the transformations of allopregnanolone and estradiol by 17beta-hydroxysteroid dehydrogenase type 10 (2018), Bioorg. Med. Chem. Lett., 28, 3554-3559 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-17alpha-methylandrostane-3alpha,17beta-diol	0.1 mM, 21.9% inhibition in the reaction with allopregnanolone. 0.3 mM, 22.6% inhibition in the reaction with 17beta-estradiol	Homo sapiens
([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-17alpha-pregn-20-yne-3alpha,17-diol	0.1 mM, 20.0% inhibition in the reaction with allopregnanolone. 0.3 mM, 44.5% inhibition in the reaction with 17beta-estradiol	Homo sapiens
17,17-difluoro-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstan-3alpha-ol	0.1 mM, 38.6% inhibition in the reaction with allopregnanolone. 0.3 mM, 13.3% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3alpha-hydroxy-3beta-([4-[(3-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)androstan-17-one	0.1 mM, 12.5% inhibition in the reaction with allopregnanolone. 0.3 mM, 31.0% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-16,16-dimethylandrostan-17-one	0.1 mM, 11.1% inhibition in the reaction with allopregnanolone. 0.3 mM, 24.6% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstan-17-one	0.1 mM, 14.7% inhibition in the reaction with allopregnanolone. 0.3 mM, 30.0% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3alpha-hydroxy-3beta-([4-[(quinolin-3-yl)methyl]piperazin-1-yl]methyl)androstan-17-one	0.1 mM, 15.2% inhibition in the reaction with allopregnanolone. 0.3 mM, 36.1% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstane-3alpha,17alpha-diol	0.1 mM, 41.7% inhibition in the reaction with allopregnanolone. 0.3 mM, 31.7% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstane-3alpha,17beta-diol	0.1 mM, no inhibition in the reaction with allopregnanolone. 0.3 mM, 13.7% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one	0.1 mM, 1.5% inhibition in the reaction with allopregnanolone	Homo sapiens
3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one	0.1 mM, 5.0% inhibition in the reaction with allopregnanolone	Homo sapiens
3beta-[[4-(4-benzoylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one	0.1 mM, 8.0% inhibition in the reaction with allopregnanolone. 0.3 mM, 58.8% inhibition in the reaction with 17beta-estradiol	Homo sapiens
3beta-[[4-([1,1'-biphenyl]-4-carbonyl)piperazin-1-yl]methyl]-3?-hydroxyandrostan-17-one	0.1 mM, 19.3% inhibition in the reaction with allopregnanolone. 0.3 mM, 29.4% inhibition in the reaction with 17beta-estradiol	Homo sapiens
4-(dimethylsulfamoyl)-N-(4-[[3alpha-hydroxy-17-oxoandrostan-beta?-yl]methyl]piperazin-1-yl)benzene-1-carbothioamide	0.1 mM, 13.3% inhibition in the reaction with allopregnanolone. 0.3 mM, 0.3% inhibition in the reaction with 17beta-estradiol	Homo sapiens
N-(4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazin-1-yl)[3-(trifluoromethyl)phenyl]ethanethioamide	0.1 mM, 34.2% inhibition in the reaction with allopregnanolone. 0.3 mM, 8.5% inhibition in the reaction with 17beta-estradiol	Homo sapiens
N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide	0.1 mM, no inhibition in the reaction with allopregnanolone. 0.3 mM, 10.2% inhibition in the reaction with 17beta-estradiol	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.015	-	allopregnanolone	pH and temperature not specified in the publication	Homo sapiens
0.043	-	17beta-estradiol	pH and temperature not specified in the publication	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
mitochondrion	-	Homo sapiens	5739	-

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q99714	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
17beta-estradiol + NAD+	-	Homo sapiens	estrone + NADH + H+	-	?
allopregnanolone + NAD+	-	Homo sapiens	5alpha-dihydroprogesterone + NADH + H+	-	?

Synonyms

Synonyms	Comment	Organism
17beta-HSD10	-	Homo sapiens
17beta-hydroxysteroid dehydrogenase type 10	-	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.011	-	17beta-estradiol	pH and temperature not specified in the publication	Homo sapiens
0.1	-	allopregnanolone	pH and temperature not specified in the publication	Homo sapiens

General Information

General Information	Comment	Organism
physiological function	by its oxidative activity, the enzyme can decrease the concentration of two important neurosteroids, allopregnanolone (ALLOP) and 17beta-estradiol, respectively preventing their neurogenesis and neuroprotective effects	Homo sapiens

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Release 2023.1 (January 2023)