Literature summary for 1.1.1.62 extracted from

Vicker, N.; Lawrence, H.R.; Allan, G.M.; Bubert, C.; Smith, A.; Tutill, H.J.; Purohit, A.; Day, J.M.; Mahon, M.F.; Reed, M.J.; Potter, B.V.
Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (2006), ChemMedChem, 1, 464-481.

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Application

Application	Comment	Organism
medicine	as estradiol stimulates the growth and development of hormone-dependent breast cancer, inhibition of the final step of its synthesis is an attractive target for the treatment of this disease	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16-methylcarboxylic acid-S-alpha-methylbenzyl amide	50% inhibition at 0.001 mM	Homo sapiens
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16alpha/beta-methylcarboxylic acid-(5-methylpyrimidinyl-2-ylmethyl)amide	37% inhibition at 0.001 mM	Homo sapiens
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16alpha/beta-methylcarboxylic acid-(pyridine-3-ylmethyl)amide	64% inhibition at 0.01 mM	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
estrone + NADPH + H+	Homo sapiens	final step in synthesis of estradiol	estradiol-17beta + NADP+	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
T-47D cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
estrone + NADPH + H+	-	Homo sapiens	estradiol-17beta + NADP+	-	?
estrone + NADPH + H+	final step in synthesis of estradiol	Homo sapiens	estradiol-17beta + NADP+	-	?

Synonyms

Synonyms	Comment	Organism
17beta-HSD1	-	Homo sapiens
17beta-hydroxysteroid dehydrogenase type 1	-	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
NADPH	-	Homo sapiens

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Release 2023.1 (January 2023)