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Literature summary extracted from

  • Ning, X.; Yang, Y.; Deng, H.; Zhang, Q.; Huang, Y.; Su, Z.; Fu, Y.; Xiang, Q.; Zhang, S.
    Development of 17beta-hydroxysteroid dehydrogenase type 3 as a target in hormone-dependent prostate cancer therapy (2017), Steroids, 121, 10-16 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.64 (2,4-dihydroxyphenyl)-phenylmethanone
-
 Homo sapiens
1.1.1.64 1-methyl-3,17-dione-androsta-1,4-diene
-
 Homo sapiens
1.1.1.64 5-(3-bromo-4-hydroxybenzyl)-3-(4-methoxyphenyl)-1,3-thiazol-2-one selective non-steroidal 17beta-HSD3 inhibitor that does not show any undesired inhibition of estrogen biosynthesis and does not possess the transcriptional activity against any of these nuclear receptors Homo sapiens
1.1.1.64 RM-532-105 the inhibitor RM-532-105 seems to have difficulty penetrating the testis and was found to be concentrated in the testicular capsule, therefore unable to inhibit the 17beta-HSD3 located inside the testis Homo sapiens
1.1.1.64 STX2171 ability to penetrate the cell. Lack of inhibition of 17beta-HSD2 (the enzyme that catalyzes the opposite reaction to that of 17beta-HSD3, which is the oxidation of active testosterone to inactive androstenedione) Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.64 microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.64 Homo sapiens P37058
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.64 blood platelet
-
 Homo sapiens
-
1.1.1.64 megakaryocyte
-
 Homo sapiens
-
1.1.1.64 prostate gland cancer cell the enzyme (17beta-HSD3) is over-expressed in hormone-dependent prostate cancer Homo sapiens
-
1.1.1.64 testis
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.64 androstenedione + NADPH + H+
-
 Homo sapiens testosterone + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.64 17beta-HSD3
-
 Homo sapiens
1.1.1.64 17beta-hydroxysteroid dehydrogenase type 3
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.64 0.0002
-
 pH and temperature not specified in the publication Homo sapiens STX2171

Expression

EC Number Organism Comment Expression
1.1.1.64 Homo sapiens in thrombocythemia, a rare myeloproliferative disorder, 17beta-HSD3 is down-regulated about 4.5fold down
1.1.1.64 Homo sapiens the enzyme (17beta-HSD3) is over-expressed in hormone-dependent prostate cancer. 17beta-HSD3 mRNA increases over 30fold in cancerous prostate biopsies and the enzyme is overexpressed 8fold in LuCaP-23 and LuCAP-35 cell lines, obtained from metastatic tissues of a patient resistant to castration therapy up

General Information

EC Number General Information Comment Organism
1.1.1.64 drug target since 17beta-HSD3 plays a central role in testosterone production, it is a promising therapeutic target to reduce the circulating level of androgens and to suppress androgen-sensitive tumor proliferation Homo sapiens