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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
androstenedione + NADPH + H+ | Homo sapiens | - |
testosterone + NADP+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P37058 | - |
- |
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 | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
androstenedione + NADPH + H+ | - |
Homo sapiens | testosterone + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
17beta-HSD3 | - |
Homo sapiens |
17beta-hydroxysteroid dehydrogenase type 3 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0002 | - |
pH and temperature not specified in the publication | Homo sapiens | STX2171 |
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 | 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 |