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Hydroxybenzothiazoles as New Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1)
Alessandro Spadaro, Matthias Negri, Sandrine Marchais-Oberwinkler, Emmanuel Bey, Martin Frotscher, and Masaru Katoh
PLoS ONE
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7 :e29252
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Design and synthesis of substrate mimetics based on an indole scaffold: potential inhibitors of 17β-HSD type 1
Štefan Starčević, Polona Božnar, Samo Turk, Stanislav Gobec, and Tea Lanišnik Rižner
Hormone Molecular Biology and Clinical Investigation
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6 :
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17ß-Hydroxysteroid dehydrogenase type 1 as predictor of tamoxifen response in premenopausal breast cancer
Ann-Christine Källström, Rebecka Salme, Lisa Rydén, Bo Nordenskjöld, Per-Ebbe Jönsson, and Olle Stål
European Journal of Cancer
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46 :892
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Curcumin derivatives inhibit testicular 17β-hydroxysteroid dehydrogenase 3
Guo-Xin Hu, Guang Liang, Yanhui Chu, Xiaokun Li, Qing-Quang Lian, Han Lin, Yi He, Yadong Huang, Dianne O. Hardy, and Ren-Shan
Ge
Bioorganic & Medicinal Chemistry Letters
(2010)
20 :2549
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Insight into the mode of action and selectivity of PBRM, a covalent steroidal inhibitor of 17β-hydroxysteroid dehydrogenase
type 1
Alexandre Trottier, René Maltais, Diana Ayan, Xavier Barbeau, Jenny Roy, Martin Perreault, Richard Poulin, Patrick Lagüe,
and Donald Poirier
Biochemical Pharmacology
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144 :149
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A role for the dehydrogenase DHRS7 (SDR34C1) in prostate cancer
Julia K. Seibert, Luca Quagliata, Cristina Quintavalle, Thomas G. Hammond, Luigi Terracciano, and Alex Odermatt
Cancer Medicine
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4 :1717
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Estrogen metabolism and action in endometriosis
Tea Lanišnik Rižner
Molecular and Cellular Endocrinology
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307 :8
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Molecular cloning and expression of 17β-hydroxysteroid dehydrogenase type 2 gene in Hu sheep
Chang Long Wang, Shi Jia Ying, Zi Yu Wang, Hui Jun Xing, Li Zhong Wang, Dong Yang He, Shen Hua Xiao, and Feng Wang
Molecular Biology Reports
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40 :1073
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Investigation of Testosterone, Androstenone, and Estradiol Metabolism in HepG2 Cells and Primary Culture Pig Hepatocytes and
Their Effects on 17βHSD7 Gene Expression
Gang Chen, Sicong Li, Xinxing Dong, Ying Bai, Ailiang Chen, Shuming Yang, Meiying Fang, Galia Zamaratskaia, Olena Doran, and
Xianglin Shi
PLoS ONE
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7 :e52255
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Identification of fused 16β,17β-oxazinone-estradiol derivatives as a new family of non-estrogenic 17β-hydroxysteroid dehydrogenase
type 1 inhibitors
René Maltais, Alexandre Trottier, Audrey Delhomme, Xavier Barbeau, Patrick Lagüe, and Donald Poirier
European Journal of Medicinal Chemistry
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93 :470
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Impact of structural modifications at positions 13, 16 and 17 of 16β-(m-carbamoylbenzyl)-estradiol on 17β-hydroxysteroid dehydrogenase
type 1 inhibition and estrogenic activity
René Maltais, Alexandre Trottier, Xavier Barbeau, Patrick Lagüe, Martin Perreault, Jean-François Thériault, Sheng-Xiang Lin,
and Donald Poirier
The Journal of Steroid Biochemistry and Molecular Biology
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161 :24
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Current knowledge of the multifunctional 17β-hydroxysteroid dehydrogenase type 1 (HSD17B1)
Wanhong He, Misra Gauri, Tang Li, Ruixuan Wang, and Sheng-Xiang Lin
Gene
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588 :54
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Synthesis and Biological Evaluation of Triazolyl 13α-Estrone–Nucleoside Bioconjugates
Brigitta Bodnár, Erzsébet Mernyák, János Wölfling, Gyula Schneider, Bianka Herman, Mihály Szécsi, Izabella Sinka, István Zupkó,
Zoltán Kupihár, and Lajos Kovács
Molecules
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21 :1212
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Impact of estradiol structural modifications (18-methyl and/or 17-hydroxy inversion of configuration) on the in vitro and
in vivo estrogenic activity
Diana Ayan, Jenny Roy, René Maltais, and Donald Poirier
The Journal of Steroid Biochemistry and Molecular Biology
(2011)
127 :324
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New cancer drugs targeting the biosynthesis of estrogens and androgens
Donald Poirier
Drug Development Research
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69 :304
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Comparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17β-hydroxysteroid
dehydrogenase type 1
Bianka Edina Herman, Johanna Szabó, Ildikó Bacsa, János Wölfling, Gyula Schneider, Mónika Bálint, Csaba Hetényi, Erzsébet
Mernyák, and Mihály Szécsi
Journal of Enzyme Inhibition and Medicinal Chemistry
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31 :61
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Regulation of 17β-hydroxysteroid dehydrogenases in cancer: regulating steroid receptor at pre-receptor stage
Mirja Rotinen, Joaquín Villar, and Ignacio Encío
Journal of Physiology and Biochemistry
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68 :461
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Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar
IC 50 for a proof-of-principle study
Ahmed S. Abdelsamie, Chris J. van Koppen, Emmanuel Bey, Mohamed Salah, Carsten Börger, Lorenz Siebenbürger, Matthias W. Laschke,
Michael D. Menger, and Martin Frotscher
European Journal of Medicinal Chemistry
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127 :944
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The effects of the standardized extracts of Ginkgo biloba on steroidogenesis pathways and aromatase activity in H295R human
adrenocortical carcinoma cells
Mijie Kim, Yong Joo Park, Huiyeon Ahn, Byeonghak Moon, Kyu Hyuck Chung, and Seung Min Oh
Environmental Health and Toxicology
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31 :e2016010
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Reprint of “In vitro and in vivo evaluation of a 3β-androsterone derivative as inhibitor of 17β-hydroxysteroid dehydrogenase
type 3”
Jenny Roy, Michelle-Audrey Fournier, René Maltais, Lucie Carolle Kenmogne, and Donald Poirier
The Journal of Steroid Biochemistry and Molecular Biology
(2015)
153 :170
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New Hormonal Therapies for Castration-Resistant Prostate Cancer
Elahe A. Mostaghel and Stephen Plymate
Endocrinology and Metabolism Clinics of North America
(2011)
40 :625
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Oestrogen and colorectal cancer: mechanisms and controversies
Paul A. Foster
International Journal of Colorectal Disease
(2013)
28 :737
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Pre-receptor steroid metabolism as target for pharmacological treatment
Jerzy Adamski
Molecular and Cellular Endocrinology
(2009)
301 :1
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The diversity of sex steroid action: novel functions of hydroxysteroid (17 ) dehydrogenases as revealed by genetically modified
mouse models
T. Saloniemi, H. Jokela, L. Strauss, P. Pakarinen, and M. Poutanen
Journal of Endocrinology
(2012)
212 :27
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Design, chemical synthesis, and in vitro biological evaluation of simplified estradiol–adenosine hybrids as inhibitors of
17β-hydroxysteroid dehydrogenase type 1
Marie Bérubé and Donald Poirier
Canadian Journal of Chemistry
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87 :1180
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Species Used for Drug Testing Reveal Different Inhibition Susceptibility for 17beta-Hydroxysteroid Dehydrogenase Type 1
Gabriele Möller, Bettina Husen, Dorota Kowalik, Leena Hirvelä, Dariusz Plewczynski, Leszek Rychlewski, Josef Messinger, Hubert
Thole, Jerzy Adamski, and Ulrich Zanger
PLoS ONE
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5 :e10969
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Convergent stereoselective and efficient synthesis of furanic-steroid derivatives
Siham Farhane, Michelle-Audrey Fournier, René Maltais, and Donald Poirier
Tetrahedron
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67 :2434
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Identification of chemically diverse, novel inhibitors of 17β-hydroxysteroid dehydrogenase type 3 and 5 by pharmacophore-based
virtual screening
Daniela Schuster, Dorota Kowalik, Johannes Kirchmair, Christian Laggner, Patrick Markt, Christel Aebischer-Gumy, Fabian Ströhle,
Gabriele Möller, Gerhard Wolber, Thomas Wilckens, Thierry Langer, Alex Odermatt, and Jerzy Adamski
The Journal of Steroid Biochemistry and Molecular Biology
(2011)
125 :148
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Identification of a First Enzymatic Activator of a 17β-Hydroxysteroid Dehydrogenase
Alexandre Trottier, René Maltais, and Donald Poirier
ACS Chemical Biology
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9 :1668
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Expression of estrogenicity genes in a lineage cell culture model of human breast cancer progression
Jiaqi Fu, Amy M. Weise, Josie L. Falany, Charles N. Falany, Bryan J. Thibodeau, Fred R. Miller, Thomas A. Kocarek, and Melissa
Runge-Morris
Breast Cancer Research and Treatment
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120 :35
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Steroid sulfatase inhibitors: Promising new tools for breast cancer therapy?
Jürgen Geisler, Hironobu Sasano, Shiuan Chen, and Atul Purohit
The Journal of Steroid Biochemistry and Molecular Biology
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125 :39
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Probing the origins of 17β-hydroxysteroid dehydrogenase type 1 inhibitory activity via QSAR and molecular docking
Kakanand Srungboonmee, Napat Songtawee, Teerawat Monnor, Virapong Prachayasittikul, and Chanin Nantasenamat
European Journal of Medicinal Chemistry
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96 :231
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Structural Basis for Species Specific Inhibition of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Computational Study
and Biological Validation
Tobias Klein, Claudia Henn, Matthias Negri, Martin Frotscher, and Bostjan Kobe
PLoS ONE
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6 :e22990
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Dienogest reduces HSD17 1 expression and activity in endometriosis
T. Mori, F. Ito, H. Matsushima, O. Takaoka, A. Koshiba, Y. Tanaka, I. Kusuki, and J. Kitawaki
Journal of Endocrinology
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225 :69
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HBCDD-induced sustained reduction in mitochondrial membrane potential, ATP and steroidogenesis in peripubertal rat Leydig
cells
Svetlana Fa, Kristina Pogrmic-Majkic, Dragana Samardzija, Jelena Hrubik, Branka Glisic, Radmila Kovacevic, and Nebojsa Andric
Toxicology and Applied Pharmacology
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282 :20
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Insights in 17β-HSD1 Enzyme Kinetics and Ligand Binding by Dynamic Motion Investigation
Matthias Negri, Maurizio Recanatini, Rolf W. Hartmann, and Floyd Romesberg
PLoS ONE
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5 :e12026
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Synthesis of a dansyl-labeled inhibitor of 17β-hydroxysteroid dehydrogenase type 3 for optical imaging
Lucie Carolle Kenmogne, René Maltais, and Donald Poirier
Bioorganic & Medicinal Chemistry Letters
(2016)
26 :2179
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Discovery of a Non-Estrogenic Irreversible Inhibitor of 17β-Hydroxysteroid Dehydrogenase Type 1 from 3-Substituted-16β-(m-carbamoylbenzyl)-estradiol
Derivatives
René Maltais, Diana Ayan, Alexandre Trottier, Xavier Barbeau, Patrick Lagüe, Jean-Emmanuel Bouchard, and Donald Poirier
Journal of Medicinal Chemistry
(2014)
57 :204
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In vitro and in vivo evaluation of a 3β-androsterone derivative as inhibitor of 17β-hydroxysteroid dehydrogenase type 3
Jenny Roy, Michelle-Audrey Fournier, René Maltais, Lucie Carolle Kenmogne, and Donald Poirier
The Journal of Steroid Biochemistry and Molecular Biology
(2014)
141 :44
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Chemical synthesis, characterisation and biological evaluation of lactonic-estradiol derivatives as inhibitors of 17β-hydroxysteroid
dehydrogenase type 1
Siham Farhane, Michelle-Audrey Fournier, and Donald Poirier
The Journal of Steroid Biochemistry and Molecular Biology
(2013)
137 :322
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A validated and rapid high-performance liquid chromatography method for the quantification of conversion of radio-labelled
sex steroids
Tove Sivik, Svante Vikingsson, Henrik Gréen, and Agneta Jansson
Hormone Molecular Biology and Clinical Investigation
(2010)
3 :
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STX2171, a 17 -hydroxysteroid dehydrogenase type 3 inhibitor, is efficacious in vivo in a novel hormone-dependent prostate
cancer model
J. M. Day, P. A. Foster, H. J. Tutill, F. Schmidlin, C. M. Sharland, J. D. Hargrave, N. Vicker, B. V. L. Potter, M. J. Reed,
and A. Purohit
Endocrine Related Cancer
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20 :53
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17β-Hydroxysteroid Dehydrogenase Type 14 Is a Predictive Marker for Tamoxifen Response in Oestrogen Receptor Positive Breast
Cancer
Tove Sivik, Cecilia Gunnarsson, Tommy Fornander, Bo Nordenskjöld, Lambert Skoog, Olle Stål, Agneta Jansson, and Tatjana Adamovic
PLoS ONE
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7 :e40568
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Bicyclic Substituted Hydroxyphenylmethanone Type Inhibitors of 17 β-Hydroxysteroid Dehydrogenase Type 1 (17 β-HSD1): The Role
of the Bicyclic Moiety
Alexander Oster, Tobias Klein, Claudia Henn, Ruth Werth, Sandrine Marchais-Oberwinkler, Martin Frotscher, and Rolf W. Hartmann
ChemMedChem
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6 :476
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Human hydroxysteroid dehydrogenases and pre-receptor regulation: Insights into inhibitor design and evaluation
Trevor M. Penning
The Journal of Steroid Biochemistry and Molecular Biology
(2011)
125 :46
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Synthesis of Two Estradiol-Imidazole C-Ribonucleoside Hybrid Compounds Exhibiting Inhibitory Effects against Type 1 17β-Hydroxysteroid
Dehydrogenase
Shinya Harusawa, Chihiro Kojima, Kensuke Fujii, Yuusaku Yamashita, Tomoya Tanaka, Lisa Araki, Toshinobu Yoshimura, Minoru
Sakaguchi, Yoshihide Usami, and Masanori Takaoka
HETEROCYCLES
(2010)
81 :2817
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Biochemical and biological evaluation of novel potent coumarin inhibitor of 17β-HSD type 1
Š. Starčević, P. Kocbek, G. Hribar, T. Lanišnik Rižner, and S. Gobec
Chemico-Biological Interactions
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191 :60
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Contribution to the development of inhibitors of 17β-hydroxysteroid dehydrogenase types 1 and 7: Key tools for studying and
treating estrogen-dependent diseases
Donald Poirier
The Journal of Steroid Biochemistry and Molecular Biology
(2011)
125 :83
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Computational investigation of the binding mode of bis(hydroxylphenyl)arenes in 17β-HSD1: molecular dynamics simulations,
MM-PBSA free energy calculations, and molecular electrostatic potential maps
Matthias Negri, Maurizio Recanatini, and Rolf W. Hartmann
Journal of Computer-Aided Molecular Design
(2011)
25 :795
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Development of 3-substituted-androsterone derivatives as potent inhibitors of 17β-hydroxysteroid dehydrogenase type 3
René Maltais, Michelle-Audrey Fournier, and Donald Poirier
Bioorganic & Medicinal Chemistry
(2011)
19 :4652
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Development of hormone-dependent prostate cancer models for the evaluation of inhibitors of 17β-hydroxysteroid dehydrogenase
Type 3
Joanna M. Day, Helena J. Tutill, Paul A. Foster, Helen V. Bailey, Wesley B. Heaton, Christopher M. Sharland, Nigel Vicker,
Barry V.L. Potter, Atul Purohit, and Michael J. Reed
Molecular and Cellular Endocrinology
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301 :251
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Structure and Mechanism of Human UDP-glucose 6-Dehydrogenase
Sigrid Egger, Apirat Chaikuad, Kathryn L. Kavanagh, Udo Oppermann, and Bernd Nidetzky
Journal of Biological Chemistry
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286 :23877
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17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: Protein structures, functions, and recent progress in
inhibitor development
Sandrine Marchais-Oberwinkler, Claudia Henn, Gabriele Möller, Tobias Klein, Matthias Negri, Alexander Oster, Alessandro Spadaro,
Ruth Werth, Marie Wetzel, Kuiying Xu, Martin Frotscher, Rolf W. Hartmann, and Jerzy Adamski
The Journal of Steroid Biochemistry and Molecular Biology
(2011)
125 :66
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Maternal lead exposure during lactation persistently impairs testicular development and steroidogenesis in male offspring
Hua Wang, Yan-Li Ji, Qun Wang, Xian-Feng Zhao, Huan Ning, Ping Liu, Cheng Zhang, Tao Yu, Ying Zhang, Xiu-Hong Meng, and De-Xiang
Xu
Journal of Applied Toxicology
(2013)
33 :1384
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Inhibition of in vitro metabolism of testosterone in human, dog and horse liver microsomes to investigate species differences
Jana Zielinski and Meike Mevissen
Toxicology in Vitro
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29 :468
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Development of 17β-hydroxysteroid dehydrogenase type 3 as a target in hormone-dependent prostate cancer therapy
Xiaohui Ning, Yan Yang, Hong Deng, Qihao Zhang, Yadong Huang, Zhijian Su, Yongmei Fu, Qi Xiang, and Shu Zhang
Steroids
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121 :10
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17β-Hydroxysteroid dehydrogenase inhibitors: a patent review
Donald Poirier
Expert Opinion on Therapeutic Patents
(2010)
20 :1123
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Structure-based design, synthesis and in vitro characterization of potent 17β-hydroxysteroid dehydrogenase type 1 inhibitors
based on 2-substitutions of estrone and D-homo-estrone
Gabriele Möller, Dominga Deluca, Christian Gege, Andrea Rosinus, Dorota Kowalik, Olaf Peters, Peter Droescher, Walter Elger,
Jerzy Adamski, and Alexander Hillisch
Bioorganic & Medicinal Chemistry Letters
(2009)
19 :6740
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Synthesis and preliminary evaluation of a modified estradiol-core bearing a fused γ-lactone as non-estrogenic inhibitor of
17β-hydroxysteroid dehydrogenase type 1
Étienne Ouellet, Diana Ayan, and Donald Poirier
Bioorganic & Medicinal Chemistry Letters
(2011)
21 :5510
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Transcriptional regulation of type 11 17β-hydroxysteroid dehydrogenase expression in prostate cancer cells
Mirja Rotinen, Joaquín Villar, Jon Celay, Irantzu Serrano, Vicente Notario, and Ignacio Encío
Molecular and Cellular Endocrinology
(2011)
339 :45
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Crucial Role of 3-Bromoethyl in Removing the Estrogenic Activity of 17β-HSD1 Inhibitor 16β-(m-Carbamoylbenzyl)estradiol
René Maltais, Diana Ayan, and Donald Poirier
ACS Medicinal Chemistry Letters
(2011)
2 :678
