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Literature summary for 1.1.1.51 extracted from

  • Tchedam Ngatcha, B.; Luu-The, V.; Labrie, F.; Poirier, D.
    Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship (2005), J. Med. Chem., 48, 5257-5268.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
overexpression in HEK-293 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3alpha-alkylated androsterone derivatives 17-88% inhibition at 0.003 mM, overview Homo sapiens
3alpha-ether-3beta-substituted androsterone derivatives diverse derivatives, IC50: 70-760 nM, overview Homo sapiens
3beta-alkylated androsterone derivatives IC50: 57-147 nM Homo sapiens
3beta-phenylethyl-3alpha-methyl-O-androsterone IC50: 73 nM Homo sapiens
3beta-phenylethyl-androsterone IC50: 99 nM Homo sapiens
3beta-phenylmethyl-androsterone IC50: 57 nM Homo sapiens
3beta-substituted androsterone derivatives IC50: 57-147 nM Homo sapiens
additional information synthesis, inhibitory potency, and in vivo effects of the diverse inhibitor derivatives, detailed overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
androst-4-ene-3,17-dione + NADPH Homo sapiens
-
testosterone + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell low enzyme expression level Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
androst-4-ene-3,17-dione + NADPH
-
Homo sapiens testosterone + NADP+
-
?

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000057
-
IC50: 57 nM Homo sapiens 3beta-phenylmethyl-androsterone
0.000057 0.000147 IC50: 57-147 nM Homo sapiens 3beta-substituted androsterone derivatives
0.000057 0.000147 IC50: 57-147 nM Homo sapiens 3beta-alkylated androsterone derivatives
0.00007 0.00076 diverse derivatives, IC50: 70-760 nM, overview Homo sapiens 3alpha-ether-3beta-substituted androsterone derivatives
0.000073
-
IC50: 73 nM Homo sapiens 3beta-phenylethyl-3alpha-methyl-O-androsterone
0.000099
-
IC50: 99 nM Homo sapiens 3beta-phenylethyl-androsterone