A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity

Human estrogenic 17beta-hydroxysteroid dehydrogenase (17beta-HSD type 1) catalyzes the final step in the synthesis of active estrogens that stimulate the proliferation of breast cancer cells. Based on the initial premise to make use of the binding energies of both the substrate and cofactor sites, a...

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Veröffentlicht in:	The FASEB journal 2002-11, Vol.16 (13), p.1829-1831
Hauptverfasser:	Qiu, Wei, Campbell, Robert L, Gangloff, Anne, Dupuis, Philippe, Boivin, Roch P, Tremblay, Martin R, Poirier, Donald, Lin, Sheng-Xiang
Format:	Artikel
Sprache:	eng
Schlagworte:	17-Hydroxysteroid Dehydrogenases - antagonists & inhibitors 17-Hydroxysteroid Dehydrogenases - chemistry 17-Hydroxysteroid Dehydrogenases - metabolism Adenosine - chemistry Adenosine - metabolism Adenosine - pharmacology Binding, Competitive Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Estradiol - chemistry Estradiol - metabolism Estradiol - pharmacology Kinetics Models, Molecular Protein Conformation
Online-Zugang:	Volltext
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