دورية أكاديمية
Substituted Aryl Benzylamines as Potent and Selective Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 3.
العنوان: | Substituted Aryl Benzylamines as Potent and Selective Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 3. |
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المؤلفون: | Vicker, Nigel, Bailey, Helen V., Day, Joanna M., Mahon, Mary F., Smith, Andrew, Tutill, Helena J., Purohit, Atul, Potter, Barry V. L. |
المصدر: | Molecules; Dec2021, Vol. 26 Issue 23, p7166, 1p |
مصطلحات موضوعية: | BENZYLAMINES, MOLECULAR docking, X-ray crystallography, CANCER cell growth, RACEMIC mixtures, SEMINAL vesicles, ANDROGEN receptors, ENANTIOMERS |
مستخلص: | 17β-Hydroxysteroid dehydrogenase type 3 (17β-HSD3) is expressed at high levels in testes and seminal vesicles; it is also present in prostate tissue and involved in gonadal and non-gonadal testosterone biosynthesis. The enzyme is membrane-bound, and a crystal structure is not yet available. Selective aryl benzylamine-based inhibitors were designed and synthesised as potential agents for prostate cancer therapeutics through structure-based design, using a previously built homology model with docking studies. Potent, selective, low nanomolar IC |
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قاعدة البيانات: | Complementary Index |
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