17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: Protein structures, functions, and recent progress in inhibitor development

Marchais-Oberwinkler, Sandrine, Henn, Claudia, Möller, Gabriele, Klein, Tobias, Negri, Matthias, Oster, Alexander, Spadaro, Alessandro, Werth, Ruth, Wetzel, Marie, Xu, Kuiying, Frotscher, Martin, Hartmann, Rolf W., Adamski, Jerzy·2011·The Journal of Steroid Biochemistry and Molecular Biology
DOI 10.1016/j.jsbmb.2010.12.013

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  15. Characterization of Recombinant Mouse Type 5 17β-Hydroxysteroid Dehydrogenase from Mus musculus and Epitestosterone Production by Its Mutant Form
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  16. BindingDB Entry 50020621: Discovery of a Novel Potent and Selective HSD17B13 Inhibitor, BI-3231, a Well-Characterized Chemical Probe Available for Open Science.
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  17. BindingDB Entry 50047937: First Structure-Activity Relationship of 17ß-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme.
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  18. BindingDB Entry 50005926: Discovery of a non-estrogenic irreversible inhibitor of 17β-hydroxysteroid dehydrogenase type 1 from 3-substituted-16β-(m-carbamoylbenzyl)-estradiol derivatives.
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  19. BindingDB Entry 50040810: Crucial Role of 3-Bromoethyl in Removing the Estrogenic Activity of 17ß-HSD1 Inhibitor 16ß-(m-Carbamoylbenzyl)estradiol.
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  20. BindingDB Entry 50045729: Identification of fused 16ß,17ß-oxazinone-estradiol derivatives as a new family of non-estrogenic 17ß-hydroxysteroid dehydrogenase type 1 inhibitors.
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  21. BindingDB Entry 50034302: Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors for the treatment of osteoporosis.
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  22. BindingDB Entry 50009394: A- and D-Ring Structural Modifications of an Androsterone Derivative Inhibiting 17β-Hydroxysteroid Dehydrogenase Type 3: Chemical Synthesis and Structure-Activity Relationships.
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  23. BindingDB Entry 50048973: Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17ß-HSD1 inhibitor with sub-nanomolar IC
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  24. BindingDB Entry 50033880: Synthesis and preliminary evaluation of a modified estradiol-core bearing a fused¿-lactone as non-estrogenic inhibitor of 17ß-hydroxysteroid dehydrogenase type 1.
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  25. BindingDB Entry 50044582: Novel, potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities.
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  26. BindingDB Entry 50034163: Triazole ring-opening leads to the discovery of potent nonsteroidal 17ß-hydroxysteroid dehydrogenase type 2 inhibitors.
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  27. BindingDB Entry 50001867: Structure-based design and profiling of novel 17β-HSD14 inhibitors.
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  28. BindingDB Entry 50006599: Synthesis of a dansyl-labeled inhibitor of 17β-hydroxysteroid dehydrogenase type 3 for optical imaging.
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  29. BindingDB Entry 50006447: Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors.
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  30. BindingDB Entry 50040559: Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17ß-HSD1.
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  31. BindingDB Entry 50044753: Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17ß-hydroxysteroid dehydrogenase type 2 inhibitors.
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  32. BindingDB Entry 50034125: Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors.
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  35. BindingDB Entry 50003057: Identification of steroidal derivatives inhibiting the transformations of allopregnanolone and estradiol by 17β-hydroxysteroid dehydrogenase type 10.
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  36. BindingDB Entry 50046704: Towards the evaluation in an animal disease model: Fluorinated 17ß-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.
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