Identification of steroidal derivatives inhibiting the transformations of allopregnanolone and estradiol by 17β-hydroxysteroid dehydrogenase type 10

[Display omitted] •Two assays were developed to assess the 17β-HSD10 inhibitory potency of compounds.•Two labeled natural steroid substrates, ALLOP and E2, were tested.•Androstane derivatives were screened and their 17β-HSD10 inhibitory activity measured.•Some compounds are dual inhibitors, and othe...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-12, Vol.28 (22), p.3554-3559
Hauptverfasser:	Boutin, Sophie, Roy, Jenny, Maltais, René, Alata, Wael, Calon, Frédéric, Poirier, Donald
Format:	Artikel
Sprache:	eng
Schlagworte:	17-Hydroxysteroid Dehydrogenases - antagonists & inhibitors 17-Hydroxysteroid Dehydrogenases - metabolism 17β-HSD10 5-alpha-Dihydroprogesterone - metabolism Allopregnanolone Alzheimer Alzheimer Disease - drug therapy Alzheimer Disease - pathology Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - therapeutic use Estradiol Estradiol - metabolism Estrone - metabolism HEK293 Cells Humans Neurosteroids Pregnanolone - metabolism Steroids - chemistry Steroids - metabolism Steroids - therapeutic use Structure-Activity Relationship
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