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Swanand Kulkarni, Yogesh Singh, Avadh Biharee, Neha Bhatia, Vikramdeep Monga & Suresh Thareja. (2023) Molecular docking, 3D-QSAR and simulation studies for identifying pharmacophoric features of indole derivatives as 17β-hydroxysteroid dehydrogenase type 5 (17β-HSD5) inhibitors. Journal of Biomolecular Structure and Dynamics 41:22, pages 12668-12685.
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Bianka Edina Herman, Johanna Szabó, Ildikó Bacsa, János Wölfling, Gyula Schneider, Mónika Bálint, Csaba Hetényi, Erzsébet Mernyák & Mihály Szécsi. (2016) Comparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17β-hydroxysteroid dehydrogenase type 1. Journal of Enzyme Inhibition and Medicinal Chemistry 31:sup3, pages 61-69.
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Philip A Carpino & Bryan Goodwin. (2010) Diabetes area participation analysis: a review of companies and targets described in the 2008 – 2010 patent literature. Expert Opinion on Therapeutic Patents 20:12, pages 1627-1651.
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Articles from other publishers (64)
Tea Lanišnik Rižner & Andrea Romano. (2023) Targeting the formation of estrogens for treatment of hormone dependent diseases–current status. Frontiers in Pharmacology 14.
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Donald Poirier. (2023) Description of Chemical Synthesis, Nuclear Magnetic Resonance Characterization and Biological Activity of Estrane-Based Inhibitors/Activators of Steroidogenesis. Molecules 28:8, pages 3499.
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Andrey K. Kirichenko, Yaroslavna V. Bardetskaya, Yuliya A. Fefelova, Kseniya V. Kotova, Victoriya O. Tokmakova & Tatyana G. Ruksha. (2023) The role of proteins implicated in skin steroidogenesis in acne vulgaris development. Vestnik dermatologii i venerologii 98:6, pages 65-72.
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Adrien Djiemeny Ngueta, Jenny Roy, René Maltais & Donald Poirier. (2023) Chemical Synthesis and Biological Evaluation of 3-Substituted Estrone/Estradiol Derivatives as 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors Acting via a Reverse Orientation of the Natural Substrate Estrone. Molecules 28:2, pages 632.
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Donald Poirier, René Maltais, Jacques A. Rousseau, Jenny Roy, Serge Phoenix, Francisco Cortés-Benítez & Roger Lecomte. (2022) Chemical synthesis of fluorinated and iodinated 17β-HSD3 inhibitors and evaluation for imaging prostate cancer tumors and tissue biodistribution. Bioorganic Chemistry 129, pages 106145.
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Abdelrahman Mohamed, Mohamed Salah, Mariam Tahoun, Manuel Hawner, Ahmed S. Abdelsamie & Martin Frotscher. (2022) Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis. Journal of Medicinal Chemistry 65:17, pages 11726-11744.
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F. Wages, P. Lentes, T. Griebenow, R. Herges, C. Peifer & E. Maser. (2022) Reduction of photoswitched, nitrogen bridged N-acetyl diazocines limits inhibition of 17βHSD3 activity in transfected human embryonic kidney 293 cells. Chemico-Biological Interactions 354, pages 109822.
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Ágnes Erika Kulmány, Bianka Edina Herman, István Zupkó, Masa Sinreih, Tea Lanišnik Rižner, Marina Savić, Aleksandar Oklješa, Andrea Nikolić, Viktória Nagy, Imre Ocsovszki, Mihály Szécsi & Suzana Jovanović-Šanta. (2021) Heterocyclic androstane and estrane d-ring modified steroids: Microwave-assisted synthesis, steroid-converting enzyme inhibition, apoptosis induction, and effects on genes encoding estrogen inactivating enzymes. The Journal of Steroid Biochemistry and Molecular Biology 214, pages 105997.
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Maxime Lespérance, Jenny Roy, Adrien Djiemeny Ngueta, René Maltais & Donald Poirier. (2021) Synthesis of 16β-derivatives of 3-(2-bromoethyl)-estra-1,3,5(10)-trien-17β-ol as inhibitors of 17β-HSD1 and/or steroid sulfatase for the treatment of estrogen-dependent diseases. Steroids 172, pages 108856.
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Francisco Cortés-Benítez, Jenny Roy, Martin Perreault, René Maltais & Donald Poirier. (2021) 16-Picolyl-androsterone derivative exhibits potent 17β-HSD3 inhibitory activity, improved metabolic stability and cytotoxic effect on various cancer cells: Synthesis, homology modeling and docking studies. The Journal of Steroid Biochemistry and Molecular Biology 210, pages 105846.
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Maria Saeed, Sajda Ashraf, Rashad Alsanosi, Hassan A. Alhazmi, Mohammed AlBratty, Asim Najmi, Asaad Khalid & Zaheer Ul-Haq. (2021) Exploring the Molecular Mechanisms of 17β-HSD5-induced Carcinogenicity of Catha edulis via Molecular Modeling Approach. Medicinal Chemistry 17:4, pages 418-428.
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Donald Poirier, Jenny Roy & René Maltais. (2021) A Targeted-Covalent Inhibitor of 17β-HSD1 Blocks Two Estrogen-Biosynthesis Pathways: In Vitro (Metabolism) and In Vivo (Xenograft) Studies in T-47D Breast Cancer Models. Cancers 13:8, pages 1841.
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Sophie Boutin, René Maltais, Jenny Roy & Donald Poirier. (2021) Synthesis of 17β-hydroxysteroid dehydrogenase type 10 steroidal inhibitors: Selectivity, metabolic stability and enhanced potency. European Journal of Medicinal Chemistry 209, pages 112909.
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Sophie Boutin, Jenny Roy, René Maltais & Donald Poirier. (2020) Formation of 5α-dihydrotestosterone from 5α-androstane-3α,17β-diol in prostate cancer LAPC-4 cells – Identifying inhibitors of non-classical pathways producing the most potent androgen. Bioorganic & Medicinal Chemistry Letters 30:2, pages 126783.
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Debbie Yancu & Thomas Sanderson. (2019) Essential oils disrupt steroidogenesis in a feto-placental co-culture model. Reproductive Toxicology 90, pages 33-43.
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Francisco Cortés-Benítez, Jenny Roy, Martin Perreault, René Maltais & Donald Poirier. (2019) A- and D-Ring Structural Modifications of an Androsterone Derivative Inhibiting 17β-Hydroxysteroid Dehydrogenase Type 3: Chemical Synthesis and Structure–Activity Relationships. Journal of Medicinal Chemistry 62:15, pages 7070-7088.
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Maxime Lespérance, Xavier Barbeau, Jenny Roy, René Maltais, Patrick Lagüe & Donald Poirier. (2018) Chemical synthesis of C3-oxiranyl/oxiranylmethyl-estrane derivatives targeted by molecular modeling and tested as potential inhibitors of 17β-hydroxysteroid dehydrogenase type 1. Steroids 140, pages 104-113.
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Tang Li, René Maltais, Donald Poirier & Sheng-Xiang Lin. (2018) Combined Biophysical Chemistry Reveals a New Covalent Inhibitor with a Low-Reactivity Alkyl Halide. The Journal of Physical Chemistry Letters 9:18, pages 5275-5280.
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René Maltais, Alexandre Trottier, Jenny Roy, Diana Ayan, Nicolas Bertrand & Donald Poirier. (2018) Pharmacokinetic profile of PBRM in rodents, a first selective covalent inhibitor of 17β-HSD1 for breast cancer and endometriosis treatments. The Journal of Steroid Biochemistry and Molecular Biology 178, pages 167-176.
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A.S. Latysheva & A.Yu. Misharin. (2018) Steroidal Inhibitors of CYP17A1 as a Template For Novel Anti-Cancer Agents Development. Biomedical Chemistry: Research and Methods 1:2, pages e00020.
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Alexandre Trottier, René Maltais, Diana Ayan, Xavier Barbeau, Jenny Roy, Martin Perreault, Richard Poulin, Patrick Lagüe & Donald Poirier. (2017) Insight into the mode of action and selectivity of PBRM, a covalent steroidal inhibitor of 17β-hydroxysteroid dehydrogenase type 1. Biochemical Pharmacology.
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Dan Xu, Juliette A. Aka, Ruixuan Wang & Sheng-Xiang Lin. (2017) 17beta-hydroxysteroid dehydrogenase type 5 is negatively correlated to apoptosis inhibitor GRP78 and tumor-secreted protein PGK1, and modulates breast cancer cell viability and proliferation. The Journal of Steroid Biochemistry and Molecular Biology 171, pages 270-280.
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Ildikó Bacsa, Rebeka Jójárt, János Wölfling, Gyula Schneider, Bianka Edina Herman, Mihály Szécsi & Erzsébet Mernyák. (2017) Synthesis of novel 13α-estrone derivatives by Sonogashira coupling as potential 17β-HSD1 inhibitors. Beilstein Journal of Organic Chemistry 13, pages 1303-1309.
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Xiaohui Ning, Yan Yang, Hong Deng, Qihao Zhang, Yadong Huang, Zhijian Su, Yongmei Fu, Qi Xiang & Shu Zhang. (2017) Development of 17β-hydroxysteroid dehydrogenase type 3 as a target in hormone-dependent prostate cancer therapy. Steroids 121, pages 10-16.
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Francisco Cortés-Benítez, Jenny Roy, René Maltais & Donald Poirier. (2017) Impact of androstane A- and D-ring inversion on 17β-hydroxysteroid dehydrogenase type 3 inhibitory activity, androgenic effect and metabolic stability. Bioorganic & Medicinal Chemistry 25:7, pages 2065-2073.
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Wei Chi, Yu Gao, Qing Hu, Wei Guo & Dapeng Li. (2017) Genome-wide analysis of brain and gonad transcripts reveals changes of key sex reversal-related genes expression and signaling pathways in three stages of Monopterus albus. PLOS ONE 12:3, pages e0173974.
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Ahmed S. Abdelsamie, Chris J. van Koppen, Emmanuel Bey, Mohamed Salah, Carsten Börger, Lorenz Siebenbürger, Matthias W. Laschke, Michael D. Menger & Martin Frotscher. (2017) 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. European Journal of Medicinal Chemistry 127, pages 944-957.
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Martin Perreault, René Maltais, Jenny Roy, Raphaël Dutour & Donald Poirier. (2017)
Design of a Mestranol 2-
N
-Piperazino-Substituted Derivative Showing Potent and Selective in vitro and in vivo Activities in MCF-7 Breast Cancer Models
. ChemMedChem 12:2, pages 177-182.
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Brigitta Bodnár, Erzsébet Mernyák, János Wölfling, Gyula Schneider, Bianka Herman, Mihály Szécsi, Izabella Sinka, István Zupkó, Zoltán Kupihár & Lajos Kovács. (2016) Synthesis and Biological Evaluation of Triazolyl 13α-Estrone–Nucleoside Bioconjugates. Molecules 21:9, pages 1212.
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Wanhong He, Misra Gauri, Tang Li, Ruixuan Wang & Sheng-Xiang Lin. (2016) Current knowledge of the multifunctional 17β-hydroxysteroid dehydrogenase type 1 (HSD17B1). Gene 588:1, pages 54-61.
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René Maltais, Alexandre Trottier, Xavier Barbeau, Patrick Lagüe, Martin Perreault, Jean-François Thériault, Sheng-Xiang Lin & Donald Poirier. (2016) 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. The Journal of Steroid Biochemistry and Molecular Biology 161, pages 24-35.
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Dan Xu & Sheng-Xiang Lin. (2016) Mimicking postmenopausal steroid metabolism in breast cancer cell culture: Differences in response to DHEA or other steroids as hormone sources. The Journal of Steroid Biochemistry and Molecular Biology 161, pages 92-100.
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Christel A.S. Bergström, William N. Charman & Christopher J.H. Porter. (2016) Computational prediction of formulation strategies for beyond-rule-of-5 compounds. Advanced Drug Delivery Reviews 101, pages 6-21.
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Lucie Carolle Kenmogne, René Maltais & Donald Poirier. (2016) Synthesis of a dansyl-labeled inhibitor of 17β-hydroxysteroid dehydrogenase type 3 for optical imaging. Bioorganic & Medicinal Chemistry Letters 26:9, pages 2179-2183.
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Keely May McNamara, Fouzia Guestini, Minako Sakurai, Kyoko Kikuchi & Hironobu Sasano. (2016) How far have we come in terms of estrogens in breast cancer? [Review]. Endocrine Journal 63:5, pages 413-424.
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Diane Fournier, Liviu Ciobanu & Donald Poirier. (2015) A Sequential Dual Cleavage of the Arylsulfamate Linker to Provide Both Sulfamate and Phenol Derivatives. Chemistry Journal of Moldova 10:2, pages 68-76.
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Xiaoqiang Wang, Catherine Gérard, Jean-François Thériault, Donald Poirier, Charles J. Doillon & Sheng-Xiang Lin. (2015) Synergistic control of sex hormones by 17β-HSD type 7: a novel target for estrogen-dependent breast cancer. Journal of Molecular Cell Biology 7:6, pages 568-579.
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Anna Vuorinen, Alex Odermatt & Daniela Schuster. (2015) Reprint of “In silico methods in the discovery of endocrine disrupting chemicals”. The Journal of Steroid Biochemistry and Molecular Biology 153, pages 93-101.
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Jenny Roy, Michelle-Audrey Fournier, René Maltais, Lucie Carolle Kenmogne & Donald Poirier. (2015) Reprint of “In vitro and in vivo evaluation of a 3β-androsterone derivative as inhibitor of 17β-hydroxysteroid dehydrogenase type 3”. The Journal of Steroid Biochemistry and Molecular Biology 153, pages 170-178.
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Guy Bertrand Djigoué, Lucie Carolle Kenmogne, Jenny Roy, René Maltais & Donald Poirier. (2015) Design, chemical synthesis and biological evaluation of 3-spiromorpholinone/3-spirocarbamate androsterone derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 3. Bioorganic & Medicinal Chemistry 23:17, pages 5433-5451.
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Maria Tsachaki, Julia Birk, Aurélie Egert & Alex Odermatt. (2015) Determination of the topology of endoplasmic reticulum membrane proteins using redox-sensitive green-fluorescence protein fusions. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research 1853:7, pages 1672-1682.
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Päivi Järvensivu, Taija Saloniemi-Heinonen, Michael Awosanya, Pasi Koskimies, Niina Saarinen & Matti Poutanen. (2015) HSD17B1 expression enhances estrogen signaling stimulated by the low active estrone, evidenced by an estrogen responsive element-driven reporter gene in vivo. Chemico-Biological Interactions 234, pages 126-134.
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René Maltais, Alexandre Trottier, Audrey Delhomme, Xavier Barbeau, Patrick Lagüe & Donald Poirier. (2015) Identification of fused 16β,17β-oxazinone-estradiol derivatives as a new family of non-estrogenic 17β-hydroxysteroid dehydrogenase type 1 inhibitors. European Journal of Medicinal Chemistry 93, pages 470-480.
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Jenny Roy, Michelle-Audrey Fournier, René Maltais, Lucie Carolle Kenmogne & Donald Poirier. (2014) In vitro and in vivo evaluation of a 3β-androsterone derivative as inhibitor of 17β-hydroxysteroid dehydrogenase type 3. The Journal of Steroid Biochemistry and Molecular Biology 141, pages 44-51.
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Andrée-Anne Hudon Thibeault, Kathy Deroy, Cathy Vaillancourt & J. Thomas Sanderson. (2014) A Unique Co-culture Model for Fundamental and Applied Studies of Human Fetoplacental Steroidogenesis and Interference by Environmental Chemicals. Environmental Health Perspectives 122:4, pages 371-377.
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René Maltais, Diana Ayan, Alexandre Trottier, Xavier Barbeau, Patrick Lagüe, Jean-Emmanuel Bouchard & Donald Poirier. (2013)
Discovery of a Non-Estrogenic Irreversible Inhibitor of 17β-Hydroxysteroid Dehydrogenase Type 1 from 3-Substituted-16β-(
m
-carbamoylbenzyl)-estradiol Derivatives
. Journal of Medicinal Chemistry 57:1, pages 204-222.
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Guy Bertrand Djigoué, Lucie Carolle Kenmogne, Jenny Roy & Donald Poirier. (2013) Synthesis of 3-spiromorpholinone androsterone derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 3. Bioorganic & Medicinal Chemistry Letters 23:23, pages 6360-6362.
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Siham Farhane, Michelle-Audrey Fournier & Donald Poirier. (2013) Chemical synthesis, characterisation and biological evaluation of lactonic-estradiol derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 1. The Journal of Steroid Biochemistry and Molecular Biology 137, pages 322-331.
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Anna Vuorinen, Alex Odermatt & Daniela Schuster. (2013) In silico methods in the discovery of endocrine disrupting chemicals. The Journal of Steroid Biochemistry and Molecular Biology 137, pages 18-26.
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Mark P. Thomas & Barry V.L. Potter. (2013) The structural biology of oestrogen metabolism. The Journal of Steroid Biochemistry and Molecular Biology 137, pages 27-49.
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Jenny Roy, Julie Lefebvre, René Maltais & Donald Poirier. (2013) Inhibition of dehydroepiandosterone sulfate action in androgen-sensitive tissues by EM-1913, an inhibitor of steroid sulfatase. Molecular and Cellular Endocrinology 376:1-2, pages 148-155.
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Lyubomir G. Nashev, Atanas G. Atanasov, Michael E. Baker & Alex Odermatt. (2013)
Cysteine-10 on 17
β
-Hydroxysteroid Dehydrogenase 1 Has Stabilizing Interactions in the Cofactor Binding Region and Renders Sensitivity to Sulfhydryl Modifying Chemicals
. International Journal of Cell Biology 2013, pages 1-8.
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Diana Ayan, René Maltais, Jenny Roy & Donald Poirier. (2012) A New Nonestrogenic Steroidal Inhibitor of 17β-Hydroxysteroid Dehydrogenase Type I Blocks the Estrogen-Dependent Breast Cancer Tumor Growth Induced by Estrone. Molecular Cancer Therapeutics 11:10, pages 2096-2104.
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Mirja Rotinen, Joaquín Villar & Ignacio Encío. (2012) Regulation of 17β-hydroxysteroid dehydrogenases in cancer: regulating steroid receptor at pre-receptor stage. Journal of Physiology and Biochemistry 68:3, pages 461-473.
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Guy-Bertrand Djigoue, Michel Simard, Lucie-Carolle Kenmogne & Donald Poirier. (2012) Two androsterone derivatives as inhibitors of androgen biosynthesis. Acta Crystallographica Section C Crystal Structure Communications 68:6, pages o231-o234.
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Alessandro Spadaro, Matthias Negri, Sandrine Marchais-Oberwinkler, Emmanuel Bey & Martin Frotscher. (2012) Hydroxybenzothiazoles as New Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1). PLoS ONE 7:1, pages e29252.
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Hsin-Yi Hung, Keduo Qian, Susan L. Morris-Natschke, Chau-Shin Hsu & Kuo-Hsiung Lee. (2012) Recent discovery of plant-derived anti-diabetic natural products. Natural Product Reports 29:5, pages 580.
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Diana Ayan, Jenny Roy, René Maltais & Donald Poirier. (2011) Impact of estradiol structural modifications (18-methyl and/or 17-hydroxy inversion of configuration) on the in vitro and in vivo estrogenic activity. The Journal of Steroid Biochemistry and Molecular Biology 127:3-5, pages 324-330.
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René Maltais, Diana Ayan & Donald Poirier. (2011)
Crucial Role of 3-Bromoethyl in Removing the Estrogenic Activity of 17β-HSD1 Inhibitor 16β-(
m
-Carbamoylbenzyl)estradiol
. ACS Medicinal Chemistry Letters 2:9, pages 678-681.
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Étienne Ouellet, Diana Ayan & Donald Poirier. (2011) Synthesis and preliminary evaluation of a modified estradiol-core bearing a fused γ-lactone as non-estrogenic inhibitor of 17β-hydroxysteroid dehydrogenase type 1. Bioorganic & Medicinal Chemistry Letters 21:18, pages 5510-5513.
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Trevor M. Penning. (2011) Human hydroxysteroid dehydrogenases and pre-receptor regulation: Insights into inhibitor design and evaluation. The Journal of Steroid Biochemistry and Molecular Biology 125:1-2, pages 46-56.
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Donald Poirier. (2011) Contribution to the development of inhibitors of 17β-hydroxysteroid dehydrogenase types 1 and 7: Key tools for studying and treating estrogen-dependent diseases. The Journal of Steroid Biochemistry and Molecular Biology 125:1-2, pages 83-94.
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Adegoke O. Adeniji, Barry M. Twenter, Michael C. Byrns, Yi Jin, Jeffrey D. Winkler & Trevor M. Penning. (2011) Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3). Bioorganic & Medicinal Chemistry Letters 21:5, pages 1464-1468.
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Sandrine Marchais-Oberwinkler, Marie Wetzel, Erika Ziegler, Patricia Kruchten, Ruth Werth, Claudia Henn, Rolf W. Hartmann & Martin Frotscher. (2010) New Drug-Like Hydroxyphenylnaphthol Steroidomimetics As Potent and Selective 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors for the Treatment of Estrogen-Dependent Diseases. Journal of Medicinal Chemistry 54:2, pages 534-547.
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