Results 11 to 20 of about 919,146 (322)

Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.

Cancer Discovery, 2018
Mutations in estrogen receptor alpha (ERα) that confer resistance to existing classes of endocrine therapies are detected in up to 30% of patients who have relapsed during endocrine treatments. Because a significant proportion of therapy-resistant breast
X. Puyang, Craig Furman, Guo-Zhu Zheng, Z. Wu, D. Banka, K. Aithal, S. Agoulnik, D. Bolduc, S. Buonamici, B. Caleb, Subhasree Das, Sean T. Eckley, P. Fekkes, M. Hao, Andrew Hart, R. Houtman, S. Irwin, J. J. Joshi, C. Karr, A. Kim, Namita Kumar, Pavan Kumar, G. Kuznetsov, W. G. Lai, N. Larsen, C. Mackenzie, L. Martin, D. Melchers, A. Moriarty, Tuong-Vi Nguyen, J. Norris, M. O’Shea, S. Pancholi, Sudeep Prajapati, S. Rajagopalan, D. Reynolds, V. Rimkunas, N. Rioux, Ricardo Ribas, Amy Y Siu, S. Sivakumar, V. Subramanian, Michael Thomas, F. Vaillancourt, John Q. Wang, S. Wardell, M. Wick, S. Yao, Lihua Yu, M. Warmuth, Peter G. Smith, P. Zhu, M. Korpal   +52 more
semanticscholar   +2 more sources

Estrogen Plus Estrogen Receptor Antagonists Alter Mineral Production by Osteoblasts In Vitro [PDF]

Hormone and Metabolic Research, 2011
In early postmenopausal women, estrogen withdrawal is associated with increased bone turnover leading to bone loss and increased risk of fracture. Recent studies have suggested that the remaining bone tissue is significantly stronger, stiff er and has an increased tissue-level mineral content.
O, Brennan, F J, O'Brien, L M, McNamara, L, McNamara   +3 more
openaire   +5 more sources

New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives [PDF]

Acta Materia Medica
Endocrine therapy that blocks estrogen receptor signaling has been effective for decades as a primary treatment choice for breast cancer patients expressing the estrogen receptor.
Jian Min, Xin Liu, Rouming Peng, Chun-Chi Chen, Wei Wang, Rey-Ting Guo   +5 more
doaj   +2 more sources

Towards β-selectivity in functional estrogen receptor antagonists [PDF]

Organic & Biomolecular Chemistry, 2012
Based on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques.
Rodríguez, José J., Filipiak, K., Maslyk, M., Ciepielski, J., Demkowicz, S., Pascual-Teresa, Sonia de, Martín-Santamaría, Sonsoles, Pascual-Teresa, Beatriz de, Ramos, Ana   +8 more
openaire   +4 more sources

β-Lactam Estrogen Receptor Antagonists and a Dual-Targeting Estrogen Receptor/Tubulin Ligand

Journal of Medicinal Chemistry, 2014
Twelve novel β-lactams were synthesized and their antiproliferative effects and binding affinity for the predominant isoforms of the estrogen receptor (ER), ERα and ERβ, were determined. β-Lactams 23 and 26 had the strongest binding affinities for ERα (IC50 values: 40 and 8 nM, respectively) and ERβ (IC50 values: 19 and 15 nM). β-Lactam 26 was the most
O'Boyle, Niamh, Pollock, Jade K, Carr, Miriam, Knox, Andrew JS, Nathwani, Seema M, Wang, Shu, Caboni, Laura, Zisterer, Daniela M, Meegan, Mary   +8 more
openaire   +7 more sources

Selective estrogen receptor modulators: tissue specificity and clinical utility

Clinical Interventions in Aging, 2014
Stephen Martinkovich,* Darshan Shah,* Sonia Lobo Planey, John A ArnottDepartment of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA*These authors contributed equally to this workAbstract: Selective estrogen receptor modulators (SERMs)
Martinkovich S, Shah D, Planey SL, Arnott JA   +3 more
doaj   +1 more source

Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists

, 2023
Herein, we report the optimization of a meta-substituted series of selective estrogen receptor degrader (SERD) antagonists for the treatment of ER+ breast cancer.
Darren Stead (2178408), Caroline McMillan (7303611), Lindsay McMurray (2068162), Dedong Wu (1738921), Bin Yang (103252), Samantha J. Hughes (1436428), Thomas A. Moss (2123341), Radoslaw Polanski (6278144), Carrie J. B. Larner (14556112), David I. Fisher (7295957), Eric T. Gangl (9436518), J. Willem M. Nissink (7424531), Christopher J. Morrow (6278141), Rodrigo J. Carbajo (264817), Kumar Thakur (1551349), Paul R. J. Davey (6278138), Mandy Lawson (1822738), Jason Breed (1398430), Natalie Cureton (14556106), Thomas A. Hunt (2642518), Nicky Whalley (14556118), Tony Johnson (1947625), Ye Wu (171928), Teresa C. M. Klinowska (14556109), Thomas M. McGuire (1638829), Tyler Grebe (1906363), Stacey Marden (9436533), Caroline Truman (112220), Daniel H. O’Donovan (7418564), James S. Scott (1398391), Elisabetta Chiarparin (1871695), Sudhir Hande (9436524), Stephen Stokes (1773739), Ryan D. Greenwood (9436521), Wenzhan Yang (8775914), Haixia Wang (173360), David Longmire (9574383), Bernard Barlaam (1638841), Michael J. Tucker (6008090), Stefan L. Kavanagh (14270979), Andrew S. Lister (9436530), Holia Hatoum-Mokdad (1637743), Dawn Trueman (14556115)   +42 more
core   +2 more sources

The Role of Sex Hormones in Degenerative Disc Disease

Global Spine Journal, 2023
Study Design Narrative review. Objectives The purpose of this review is to outline the role of sex hormones, particularly estrogen, in the pathogenesis of degenerative disc disease (DDD).
Tara Shelby BS, Emily S. Mills MD, Andy Ton BS, Jeffrey C. Wang MD, Raymond J. Hah MD, Sheeraz A. Qureshi MD, Ram K. Alluri MD   +6 more
doaj   +1 more source

Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells

eLife, 2022
Chemical manipulation of estrogen receptor alpha ligand binding domain structural mobility tunes receptor lifetime and influences breast cancer therapeutic activities.
David J Hosfield, Sandra Weber, Nan-Sheng Li, Madline Sauvage, Carstyn F Joiner, Govinda R Hancock, Emily A Sullivan, Estelle Ndukwe, Ross Han, Sydney Cush, Muriel Lainé, Sylvie C Mader, Geoffrey L Greene, Sean W Fanning   +13 more
doaj   +1 more source

Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges.

Journal of Medicinal Chemistry, 2023
Estrogen receptor alpha (ERα) is a well-established therapeutic target for the treatment of ER-positive (ER+) breast cancers. Despite the tremendous successes achieved with tamoxifen, a selective ER modulator, and aromatase inhibitors (AIs), resistance ...
R. Rej, J. E. Thomas, R. Acharyya, J. Rae, Shaomeng Wang   +4 more
semanticscholar   +1 more source