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Literature summary for 1.1.1.51 extracted from

  • Kenmogne, L.C.; Maltais, R.; Poirier, D.
    Synthesis of a dansyl-labeled inhibitor of 17beta-hydroxysteroid dehydrogenase type 3 for optical imaging (2016), Bioorg. Med. Chem. Lett., 26, 2179-2183.
    View publication on PubMed

Application

Application Comment Organism
drug development the steroidogenic enzyme 17beta-hydroxysteroid dehydrogenase type 3 (17beta-HSD3) is a therapeutic target in the management of androgen-sensitive diseases such as prostate cancer and benign prostate hyperplasia Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3a,5a)-3-[[(2R,5S)-4-[[5-(dimethylamino)naphthalen-1-yl]sulfonyl]-2,5-dimethylpiperazin-1-yl]methyl]-17-methylideneandrostan-3-ol
-
Homo sapiens
(3alpha,5alpha)-3-([(2R,5S)-2,5-dimethyl-4-[2-(trifluoromethyl)benzene-1-sulfonyl]piperazin-1-yl]methyl)-3-hydroxyandrostan-17-one i.e. RM-532-105 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
testosterone + NADP+ Homo sapiens
-
androstenedione + NADPH + H+
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
LNCaP cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
testosterone + NADP+
-
Homo sapiens androstenedione + NADPH + H+
-
r

Synonyms

Synonyms Comment Organism
17beta-HSD3
-
Homo sapiens
17beta-hydroxysteroid dehydrogenase type 3
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000085
-
pH and temperature not specified in the publication Homo sapiens (3alpha,5alpha)-3-([(2R,5S)-2,5-dimethyl-4-[2-(trifluoromethyl)benzene-1-sulfonyl]piperazin-1-yl]methyl)-3-hydroxyandrostan-17-one
0.000262
-
pH and temperature not specified in the publication Homo sapiens (3a,5a)-3-[[(2R,5S)-4-[[5-(dimethylamino)naphthalen-1-yl]sulfonyl]-2,5-dimethylpiperazin-1-yl]methyl]-17-methylideneandrostan-3-ol