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BioAssay: AID 629852

Displacement of [3H]E2 from human recombinant ERalpha by liquid scintillation counting relative to E2

Estrogen deficiency in postmenopausal women or elderly men is often associated with the skeletal disease osteoporosis. The supplementation of estradiol (E2) in osteoporotic patients is known to prevent bone fracture but cannot be administered because of adverse effect. As 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) oxidizes E2 to its inactive form estrone (E1) and has been found in more ..
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 Tested Compounds
 Tested Compounds
All(9)
 
 
Unspecified(9)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Unspecified(9)
 
 
 Related BioAssays
 Related BioAssays
AID: 629852
Data Source: ChEMBL (787300)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Estrogen receptor; Short=ER; AltName: Full=ER-alpha; AltName: Full=Estradiol receptor; AltName: Full=Nuclear receptor subfamily 3 group A member 1
Description ..   
Protein Family: Ligand binding domain of Estrogen receptor, which are activated by the hormone 17beta-estradiol (estrogen)
Comment ..   

Gene:ESR1     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) inhibitors.

Abstract: Estrogen deficiency in postmenopausal women or elderly men is often associated with the skeletal disease osteoporosis. The supplementation of estradiol (E2) in osteoporotic patients is known to prevent bone fracture but cannot be administered because of adverse effect. As 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) oxidizes E2 to its inactive form estrone (E1) and has been found in osteoblastic cells, it is an attractive target for the treatment of osteoporosis. Twenty-one novel, naphthalene-derived compounds have been synthesized and evaluated for their 17beta-HSD2 inhibition and their selectivity toward 17beta-HSD1 and the estrogen receptors (ERs) alpha and beta. Compound 19 turned out to be the most potent and selective inhibitor of 17beta-HSD2 in cell-free assays and had a very good cellular activity in MDA-MB-231 cells, expressing naturally 17beta-HSD2. It also showed marked inhibition of the E1-formation by the rat and mouse orthologous enzymes and strong inhibition of monkey 17beta-HSD2. It is thus an appropriate candidate to be further evaluated in a disease-oriented model.
(PMID: 21972996)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
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