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Literature summary for 1.1.1.51 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
Search for more literature for 1.1.1.51

Inhibitors

Inhibitors Comment Organism Structure
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
androstenedione
-
 Rattus norvegicus
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

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
NADP+
-
 Rattus norvegicus
NADPH
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000026
-
 pH 7.4, 37°C, inhibition in recombinant HEK-293 cells overexpressing 17 beta-HSD3, overview Rattus norvegicus RM-532-105
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
0.0001
-
 pH 7.4, 37°C, inhibition in wild-type rat testis, overview Rattus norvegicus RM-532-105
0.000337 0.000341 pH 7.4, 37°C Rattus norvegicus androstenedione

General Information

General Information Comment Organism
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