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Literature summary extracted from

  • Roy, J.; Fournier, M.A.; Maltais, R.; Kenmogne, L.C.; Poirier, D.
    In vitro and in vivo evaluation of a 3beta-androsterone derivative as inhibitor of 17beta-hydroxysteroid dehydrogenase type 3 (2014), J. Steroid Biochem. Mol. Biol., 141, 44-51.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.51 1-[(3R,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-2',17-dioxohexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-3,5'-[1,3]oxazolidin]-3'-yl]-3-(morpholin-4-yl)propan-2-yl cyclohexanecarboxylate D-5-2 Rattus norvegicus
1.1.1.51 androstenedione
-
 Rattus norvegicus
1.1.1.51 RM-532-105 3beta-(o-trifluoromethylphenyl-sulfonyl-dimethylpipera-zino)-androsterone, a 3 beta-dimethylpiperazino-ADT sulfonamide derivative. RM-532-105 is a better competitor of labeled enzyme substrate [14C]-4-dione than the unlabeled natural substrate 4-dione (IC50 = 341 and 337 nM) used itself as an inhibitor Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.51 microsome
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.51 testosterone + NADP+ Rattus norvegicus
-
 androstenedione + NADPH + H+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.51 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.51 testis
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.51 testosterone + NADP+
-
 Rattus norvegicus androstenedione + NADPH + H+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.51 17 beta-HSD3
-
 Rattus norvegicus
1.1.1.51 17beta-HSD3
-
 Rattus norvegicus
1.1.1.51 17beta-hydroxysteroid dehydrogenase type 3
-
 Rattus norvegicus
1.1.1.51 HSD17B3
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.51 37
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.51 7.4
-
 assay at Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.51 NADP+
-
 Rattus norvegicus
1.1.1.51 NADPH
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.51 0.000026
-
 pH 7.4, 37°C, inhibition in recombinant HEK-293 cells overexpressing 17 beta-HSD3, overview Rattus norvegicus RM-532-105
1.1.1.51 0.000037 0.000051 pH 7.4, 37°C Rattus norvegicus 1-[(3R,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-2',17-dioxohexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-3,5'-[1,3]oxazolidin]-3'-yl]-3-(morpholin-4-yl)propan-2-yl cyclohexanecarboxylate
1.1.1.51 0.0001
-
 pH 7.4, 37°C, inhibition in wild-type rat testis, overview Rattus norvegicus RM-532-105
1.1.1.51 0.000337 0.000341 pH 7.4, 37°C Rattus norvegicus androstenedione

General Information

EC Number General Information Comment Organism
1.1.1.51 physiological function 17beta-hydroxysteroid dehydrogenase type 3 catalyzes the last step in the biosynthesis of the potent androgen testosterone by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor Rattus norvegicus