Mutational Studies on 17β-HSD14, Serial Synchrotron X-ray Crystallography, Solubility Enhancement using Cyclodextrins and Fragment-Based Drug Discovery …
M Badran - 2020 - archiv.ub.uni-marburg.de
The first topic of this thesis (Chapter 2) presents a mutational study performed on 17β-
hydroxysteroid dehydrogenase type 14 (17β-HSD14) S205 variant. Five different mutations …
hydroxysteroid dehydrogenase type 14 (17β-HSD14) S205 variant. Five different mutations …
Structure-based design and profiling of novel 17β-HSD14 inhibitors
F Braun, N Bertoletti, G Möller, J Adamski… - European Journal of …, 2018 - Elsevier
The human enzyme 17β-hydroxysteroid dehydrogenase 14 (17β-HSD14) oxidizes the
hydroxyl group at position 17 of estradiol and 5-androstenediol using NAD+ as cofactor …
hydroxyl group at position 17 of estradiol and 5-androstenediol using NAD+ as cofactor …
Structural Characterization of 17β-Hydroxysteroid Dehydrogenase Type 14 and Inhibitor Optimization Using Crystallography and Computational Techniques
N Bertoletti - 2018 - archiv.ub.uni-marburg.de
17β-Hydroxysteroid dehydrogenase type 14 (17β-HSD14) is the latest identified subtype of
17β HSDs. In vivo this enzyme oxidizes the hydroxyl group at position 17 of estradiol (E2) …
17β HSDs. In vivo this enzyme oxidizes the hydroxyl group at position 17 of estradiol (E2) …
First structure–activity relationship of 17β-hydroxysteroid dehydrogenase type 14 nonsteroidal inhibitors and crystal structures in complex with the enzyme
F Braun, N Bertoletti, G Möller… - Journal of Medicinal …, 2016 - ACS Publications
17β-HSD14 belongs to the SDR family and oxidizes the hydroxyl group at position 17 of
estradiol and 5-androstenediol using NAD+ as cofactor. The goal of this study was to identify …
estradiol and 5-androstenediol using NAD+ as cofactor. The goal of this study was to identify …
Structure-based drug design of 11β-hydroxysteroid dehydrogenase type 1 inhibitors
JE Adie - 2010 - era.ed.ac.uk
The enzyme 11β-Hydroxysteroid Dehydrogenase 1 (11β-HSD1) catalyses the intracellular
biosynthesis of the active glucocorticoid cortisol. Tissue specific dysregulation of the enzyme …
biosynthesis of the active glucocorticoid cortisol. Tissue specific dysregulation of the enzyme …
Discovery of novel inhibitors of 11β-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling
H Yang, W Dou, J Lou, Y Leng, J Shen - Bioorganic & medicinal chemistry …, 2008 - Elsevier
11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is a potential target for treatment of
diabetes and metabolic syndrome. Docking and pharmacophore modeling have been used …
diabetes and metabolic syndrome. Docking and pharmacophore modeling have been used …
[PDF][PDF] Lamya H. Al-Wahaibi1, Jacques Joubert2, Olivier Blacque3, Nora H. Al-Shaalan1 &
AA El-Emam - academia.edu
5-(Adamantan-1-yl)-3-[(4-chlorobenzyl) sulfanyl]-4-methyl-4H-1, 2, 4-triazole (4) was
identified as a potential 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor and …
identified as a potential 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor and …
Structural basis for species specific inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1): computational study and biological validation
T Klein, C Henn, M Negri, M Frotscher - PLoS One, 2011 - journals.plos.org
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of estrone to
estradiol, which is the most potent estrogen in humans. Inhibition of 17β-HSD1 and thereby …
estradiol, which is the most potent estrogen in humans. Inhibition of 17β-HSD1 and thereby …
Structure-based virtual screening for identification of novel 11β-HSD1 inhibitors
H Yang, Y Shen, J Chen, Q Jiang, Y Leng… - European journal of …, 2009 - Elsevier
Structure-based pharmacophore models were built by using LigandScout and used for
virtual screening of the SPECS database to identify new potential 11β-HSD1 inhibitors. As a …
virtual screening of the SPECS database to identify new potential 11β-HSD1 inhibitors. As a …
[PDF][PDF] Identification of Novel Inhibitors of 11b-Hydroxysteroid Dehydrogenase Type 1from Natural Products Library through Docking and Pharmacophore Modeling
SCB Kotte, VK Tulam, S Raghavan… - Int. J. Res. Pharm …, 2012 - researchgate.net
To identify novel inhibitors of 11 β-HSD1 by using a structural library of custom built in-house
natural compounds database, as a refinement of the results obtained from virtual 3D …
natural compounds database, as a refinement of the results obtained from virtual 3D …