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Literature summary for 1.1.1.64 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

Inhibitors Comment Organism Structure
(2,4-dihydroxyphenyl)-phenylmethanone
-
Homo sapiens
1-methyl-3,17-dione-androsta-1,4-diene
-
Homo sapiens
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
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
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

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P37058
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

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

Expression

Organism Comment Expression
Homo sapiens in thrombocythemia, a rare myeloproliferative disorder, 17beta-HSD3 is down-regulated about 4.5fold down
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

General Information Comment Organism
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