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Expert Opinion on Therapeutic Patents Volume 20, 2010 - Issue 4
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Reviews

Estrogen receptor β selective nonsteroidal estrogens: seeking clinical indications

Michael L Mohler Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Ramesh Narayanan Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Christopher C Coss Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Kejiang Hu Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Yali He Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Zhongzhi Wu Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Seoung-Soo Hong Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Dong Jin Hwang Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
,
Duane D Miller Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA
&
James T Dalton Vice President, Preclinical Research and Development, GTx, Inc., 3 North Dunlap Street, Memphis, TN 38163, USA +1 901 507 8604; +1 901 844 8078; [email protected]
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Pages 507-534 | Published online: 20 Mar 2010

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Ilaria Paterni, Simone Bertini, Carlotta Granchi, Marco Macchia & Filippo Minutolo. (2013) Estrogen receptor ligands: a patent review update. Expert Opinion on Therapeutic Patents 23:10, pages 1247-1271.
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Articles from other publishers (21)

Anita Marfavi, Poya Kavianpour & Louis M. Rendina. (2022) Carboranes in drug discovery, chemical biology and molecular imaging. Nature Reviews Chemistry 6:7, pages 486-504.
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Ananya Banerjee, Shurui Cai, Guozhen Xie, Na Li, Xuetao Bai, Kousalya Lavudi, Kevin Wang, Xiaoli Zhang, Junran Zhang, Srinivas Patnaik, Floor J. Backes, Chad Bennett & Qi-En Wang. (2022) A Novel Estrogen Receptor β Agonist Diminishes Ovarian Cancer Stem Cells via Suppressing the Epithelial-to-Mesenchymal Transition. Cancers 14:9, pages 2311.
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David Sedlák, Tyler A. Wilson, Werner Tjarks, Hanna S. Radomska, Hongyan Wang, Jayaprakash Narayana Kolla, Zbigniew J. Leśnikowski, Alena Špičáková, Tehane Ali, Keisuke Ishita, Liva Harinantenaina Rakotondraibe, Sandip Vibhute, Dasheng Wang, Pavel Anzenbacher, Chad Bennett, Petr Bartunek & Christopher C. Coss. (2021) Structure–Activity Relationship of para -Carborane Selective Estrogen Receptor β Agonists . Journal of Medicinal Chemistry 64:13, pages 9330-9353.
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Miriam Carr, Andrew J.S. Knox, Daniel K. Nevin, Niamh O'Boyle, Shu Wang, Billy Egan, Thomas McCabe, Brendan Twamley, Daniela M. Zisterer, David G. Lloyd & Mary J. Meegan. (2020) Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. Bioorganic & Medicinal Chemistry 28:5, pages 115261.
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Rajeev Jaundoo, Jonathan Bohmann, Gloria E Gutierrez, Nancy Klimas, Gordon Broderick & Travis J A Craddock. (2020) Towards a Treatment for Gulf War Illness: A Consensus Docking Approach. Military Medicine 185:Supplement_1, pages 554-561.
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Hyejin Park, Joseph D. McEachonIIII & Julie A. Pollock. (2019) Synthesis and characterization of hydrogen peroxide activated estrogen receptor beta ligands. Bioorganic & Medicinal Chemistry 27:10, pages 2075-2082.
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Shigeru Yonekubo, Nobuhiko Fushimi, Takashi Miyagi, Osamu Nakanishi, Kenji Katsuno, Motoyasu Ozawa, Chiaki Handa, Noritaka Furuya & Hideyuki Muranaka. (2016) Synthesis and structure–activity relationships of 1-benzylindane derivatives as selective agonists for estrogen receptor beta. Bioorganic & Medicinal Chemistry 24:22, pages 5895-5910.
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Anna J. Khalaj, Jonathan Hasselmann, Catherine Augello, Spencer Moore & Seema K. Tiwari-Woodruff. (2016) Nudging oligodendrocyte intrinsic signaling to remyelinate and repair: Estrogen receptor ligand effects. The Journal of Steroid Biochemistry and Molecular Biology 160, pages 43-52.
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Eric R. Prossnitz & Jeffrey B. Arterburn. (2015) International Union of Basic and Clinical Pharmacology. XCVII. G Protein–Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacological Reviews 67:3, pages 505-540.
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Emma Shtivelman, Tomasz M. Beer & Christopher P. Evans. (2014) Molecular pathways and targets in prostate cancer. Oncotarget 5:17, pages 7217-7259.
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Karen Kar-Loen Chan, Thomas Ho-Yin Leung, David Wai Chan, Na Wei, Grace Tak-Yi Lau, Stephanie Si Liu, Michelle K-Y Siu & Hextan Yuen-Sheung Ngan. (2014) Targeting estrogen receptor subtypes (ERα and ERβ) with selective ER modulators in ovarian cancer. Journal of Endocrinology 221:2, pages 325-336.
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Konstantin Yakimchuk, Mikael Jondal & Sam Okret. (2013) Estrogen receptor α and β in the normal immune system and in lymphoid malignancies. Molecular and Cellular Endocrinology 375:1-2, pages 121-129.
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A. Cleve, K.-H. Fritzemeier, B. Haendler, N. Heinrich, C. Möller, W. Schwede & T. Wintermantel. 2012. Sex and Gender Differences in Pharmacology. Sex and Gender Differences in Pharmacology 543 587 .
J.A. Clark, S. Alves, C. Gundlah, B. Rocha, E.T. Birzin, S.-J. Cai, R. Flick, E. Hayes, K. Ho, S. Warrier, L. Pai, J. Yudkovitz, R. Fleischer, L. Colwell, S. Li, H. Wilkinson, J. Schaeffer, R. Wilkening, E. Mattingly, M. Hammond & S.P. Rohrer. (2012) Selective estrogen receptor-beta (SERM-beta) compounds modulate raphe nuclei tryptophan hydroxylase-1 (TPH-1) mRNA expression and cause antidepressant-like effects in the forced swim test. Neuropharmacology 63:6, pages 1051-1063.
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Erin K. Shanle, John R. Hawse & Wei Xu. (2011) Generation of stable reporter breast cancer cell lines for the identification of ER subtype selective ligands. Biochemical Pharmacology 82:12, pages 1940-1949.
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Stefan Nilsson, Konrad F. Koehler & Jan-Åke Gustafsson. (2011) Development of subtype-selective oestrogen receptor-based therapeutics. Nature Reviews Drug Discovery 10:10, pages 778-792.
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Lee R. Roberts, Duncan Armor, Carolyn Barker, Andrew Bent, Kirstin Bess, Alan Brown, David A. Favor, David Ellis, Stephen L. Irving, Malcolm MacKenny, Chris Phillips, Nick Pullen, Adam Stennett, Linda Strand & Michelle Styles. (2011) Sulfonamides as selective oestrogen receptor β agonists. Bioorganic & Medicinal Chemistry Letters 21:19, pages 5680-5683.
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Yoshiya Horimoto, Johan Hartman, Julie Millour, Steven Pollock, Yolanda Olmos, Ka-Kei Ho, R. Charles Coombes, Matti Poutanen, Sari I. Mäkelä, Mona El-Bahrawy, Valerie Speirs & Eric W.-F. Lam. (2011) ERβ1 Represses FOXM1 Expression through Targeting ERα to Control Cell Proliferation in Breast Cancer. The American Journal of Pathology 179:3, pages 1148-1156.
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K Yakimchuk, M Iravani, M S Hasni, P Rhönnstad, S Nilsson, M Jondal & S Okret. (2011) Effect of ligand-activated estrogen receptor β on lymphoma growth in vitro and in vivo. Leukemia 25:7, pages 1103-1110.
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Simone Bertini, Andrea De Cupertinis, Carlotta Granchi, Barbara Bargagli, Tiziano Tuccinardi, Adriano Martinelli, Marco Macchia, Jillian R. Gunther, Kathryn E. Carlson, John A. Katzenellenbogen & Filippo Minutolo. (2011) Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes. European Journal of Medicinal Chemistry 46:6, pages 2453-2462.
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Mamoun Younes & Naoko Honma. (2011) Estrogen Receptor β. Archives of Pathology & Laboratory Medicine 135:1, pages 63-66.
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