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Literature summary for 1.1.1.62 extracted from

  • Tremblay, M.R.; Boivin, R.P.; Luu-The, V.; Poirier, D.
    Inhibitors of type 1 17beta-hydroxysteroid dehydrogenase with reduced estrogenic activity: modifications of the positions 3 and 6 of estradiol (2005), J. Enzyme Inhib. Med. Chem., 20, 153-163.
    View publication on PubMed
Search for more literature for 1.1.1.62

Application

Application Comment Organism
medicine type 1 17beta-hydroxysteroid dehydrogenase is an interesting biological target for designing drugs for the treatment of estrogen-sensitive diseases such as breast cancer Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
HEK-293 cells transfected with human 17beta-HSD1-cDNA Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-(hexylsulfanyl)estra-1(10),2,4-triene-3,17beta-diol 30% inhibition at 0.001 mM, reduction of estrone with NADH as cofactor Homo sapiens
estrone 92% inhibition at 0.001 mM, IC50: 0.00009 mM Homo sapiens
N-butyl-6-[[(6beta,17beta)-17-hydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide 38% inhibition at 0.001 mM, reduction of estrone with NADH as cofactor Homo sapiens
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]oxy]-N-methylhexanamide 73% inhibition at 0.001 mM, IC50: 0.0008 mM, reduction of estrone with NADH as cofactor Homo sapiens
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide 92% inhibition at 0.001 mM, IC50: 0.00016 mM, reduction of estrone with NADH as cofactor Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
estrone + NAD(P)H + H+ Homo sapiens type 1 17beta-hydroxysteroid dehydrogenase plays a critical role in the biosynthesis of estradiol estradiol-17beta + NAD(P)+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone + NAD(P)H + H+ type 1 17beta-hydroxysteroid dehydrogenase plays a critical role in the biosynthesis of estradiol Homo sapiens estradiol-17beta + NAD(P)+
-
 ?
estrone + NADH + H+
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 Homo sapiens estradiol-17beta + NAD+
-
 ?

Synonyms

Synonyms Comment Organism
17beta-HSD
-
 Homo sapiens
type 1 17beta-hydroxysteroid dehydrogenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00009
-
 92% inhibition at 0.001 mM, IC50: 0.00009 mM Homo sapiens estrone
0.00016
-
 92% inhibition at 0.001 mM, IC50: 0.00016 mM, reduction of estrone with NADH as cofactor Homo sapiens N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
0.0008
-
 73% inhibition at 0.001 mM, IC50: 0.0008 mM, reduction of estrone with NADH as cofactor Homo sapiens N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]oxy]-N-methylhexanamide