Estrogen Receptors as Therapeutic Targets in Breast Cancer

Recent Developments in Medicinal Chemistry and Therapeutic Potential of Anti-Cancer PROTACs-Based Molecules

Khan, M. Z. I., Nazli, A., Pan, Y., & Chen, J. (2022) · Current Medicinal Chemistry · doi:10.2174/0929867329666220803112409 · Cited by 7

‘tieredScreen’ – Layered Virtual Screening Tool for the Identification of Novel Estrogen Receptor Alpha Modulators

Yang, Y., Carta, G., Peters, M. B., Price, T., O’Boyle, N. M., Knox, A. J. S., Fayne, D., Williams, D. C., Meegan, M. J., & Lloyd, D. G. (2010) · Molecular Informatics · doi:10.1002/minf.201000034 · Cited by 6

Comparison of two structurally diverse glucocorticoid receptor agonists: Cortivazol selectively regulates a distinct set of genes separate from dexamethasone in CEM cells

Miller, A. L., Webb, M. S., & Thompson, E. B. (2007) · Steroids · doi:10.1016/j.steroids.2007.05.004 · Cited by 6

ESRRG-controlled downregulation of KCNN1 in primary sensory neurons is required for neuropathic pain

Wang, H., Zuo, W., Feng, X., et al. (2024) · JCI Insight · doi:10.1172/jci.insight.180085 · Cited by 5

Identification and characterization of lipopolysaccharide binding protein (LBP) as an estrogen receptor α specific serum biomarker

Chisamore, M. J., Hong, K.-L. K., Cheng, C., et al. (2012) · Biomarkers · doi:10.3109/1354750x.2012.654406 · Cited by 5

Bioactive Natural Products for Breast Cancer Chemoprevention and Treatment

Mokashi, A., & Bhatia, N. M. (2023) · Current Bioactive Compounds · doi:10.2174/1573407219666230529151351 · Cited by 5

Involvement of glycogen debranching enzyme in bladder cancer

Weinhaus, B., & Guin, S. (2017) · Biomedical Reports · doi:10.3892/br.2017.907 · Cited by 5

Mechanisms of Drug Resistance and Use of Nanoparticle Delivery to Overcome Resistance in Breast Cancers

Beyaz, H., Uludağ, H., Kavaz, D., & Rizaner, N. (2021) · Advances in experimental medicine and biology · doi:10.1007/5584_2021_648 · Cited by 5

Design, synthesis and antiproliferative activity of raloxifene/histone deacetylase inhibitor hybrids in breast cancer

Wang, Y., Sauvage, M., Diennet, M., Weber, S., Mader, S., & Gleason, J. L. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116533 · Cited by 4

Determination of Structural Factors Contributing to Protection of Zinc Fingers in Estrogen Receptor α through Molecular Dynamic Simulations

Lutz, P. B., Coombs, W. R., & Bayse, C. A. (2025) · The Journal of Physical Chemistry B · doi:10.1021/acs.jpcb.4c05730 · Cited by 5

The Pattern of Proline, Glutamic Acid, and Leucine-Rich Protein 1 Expression in Chinese Women with Primary Breast Cancer

Zhang, Y., Wang, P., Shi, M., et al. (2014) · The International Journal of Biological Markers · doi:10.5301/jbm.5000078 · Cited by 4

In silico identification of novel inhibitors targeting the DNA-binding domain of the human estrogen receptor alpha

Cao, H., Sun, Y., Wang, L., Pan, Y., Li, Z., & Liang, Y. (2021) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2021.105966 · Cited by 4

X-ray crystallography study and optimization of novel benzothiophene analogs as potent selective estrogen receptor covalent antagonists (SERCAs) with improved potency and safety profiles

Bai, C., Lv, Y., Xiong, S., et al. (2023) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2023.106919 · Cited by 4

HDAC7 influences ER-⍺ transcription via NCoR-HDAC3 dissociation

Kodikara, I. K. M., Nwanelo, V. O., Belanger, A. K., & Pflum, M. K. H. (2025) · Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics · doi:10.1016/j.bbapap.2025.141083 · Cited by 3

Estrogen-Receptor-Related Receptors and Hormone-Dependent Cancers

Lanvin, O., Bianco, S., & Vanacker, J.-M. (2008) · Advances in experimental medicine and biology · doi:10.1007/978-0-387-69080-3_22 · Cited by 3

Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen

Marzouk, M. A., Greco, S., Gbahou, F., Küblbeck, J., Labani, N., Jockers, R., Holzgrabe, U., Wiesmüller, L., & Zlotos, D. P. (2024) · ACS Omega · doi:10.1021/acsomega.4c08881 · Cited by 4

Anti-Breast Cancer Terpenoids of Natural Origins

Negi, A. S. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-821277-6.00003-9 · Cited by 3

Assessing Estrogenic Activity of Classical Estrogen Receptor-Binding Compounds

Pepermans, R. A., & Prossnitz, E. R. (2022) · Methods in molecular biology · doi:10.1007/978-1-0716-1920-9_12 · Cited by 3

Tamoxifen therapy benefit predictive signature combining with prognostic signature in surgical‐only ER‐positive breast cancer

Lv, F., Jin, W., Zhang, X., et al. (2018) · Journal of Cellular Physiology · doi:10.1002/jcp.27756 · Cited by 3

Insights into impact of polar protic and aprotic solvents on bioactive features of 3-(Dimethylaminomethyl)-5-nitroindole: A DFT study and molecular dynamics simulations

Koyambo-Konzapa, S., Vamhindi, B. S. D. R., Khudaykulov, B., Sidhom, P. A., Khan, S., Abdelbacki, A. M. M., Abdelrahman, A. H. M., & Ibrahim, M. A. A. (2025) · PLoS ONE · doi:10.1371/journal.pone.0330941 · Cited by 2

Steroid Receptor Coactivators (SRCs) as Integrators of Multiple Signaling Pathways in Cancer Progression

Long, W., & O’Malley, B. W. (2013) · Cancer drug discovery and develogment/Cancer drug discovery and development · doi:10.1007/978-1-4614-8039-6_1 · Cited by 2

Hormonal therapy

De, S. K. (2023) · Elsevier eBooks · doi:10.1016/b978-0-443-13312-1.00006-4 · Cited by 2

Animal Models for Breast Cancer Prevention Research

Wang, C., & Brown, P. H. (2011) · Springer eBooks · doi:10.1007/978-0-387-69805-2_24 · Cited by 2

Estrogen Receptor Pathways and Breast Cancer

Peng, J., & Jordan, V. C. (2008) · Humana Press eBooks · doi:10.1007/978-1-59745-470-4_9 · Cited by 2

Estudos in silico no planejamento de candidatos a novos fármacos na terapia do câncer de mama e de reposição hormonal

Salum, L. D. B. (2007) · doi:10.11606/d.76.2007.tde-09042008-121318 · Cited by 2

Development of concise two-step catalytic approach towards lasofoxifene precursor nafoxidine

Seechurn, C. C. C. J., Smilović, I. G., Colacot, T. J., Zanotti‐Gerosa, A., & Časar, Z. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.04.021 · Cited by 2

Functional, Pharmacogenomic, and Immune Landscapes of Long Non‐Coding RNAs in Cancer

Wang, R., Luo, M., Liu, Y., Yang, H. J., Chen, Y., Chen, C., Ma, L., Ding, S., Wengler, J., Zang, Y., et al. (2025) · Advanced Science · doi:10.1002/advs.202513414 · Cited by 1

Roles and Mechanisms of Estrogen and Estrogen Receptors in Breast Cancer Resistant to Chemotherapy

Fan, W., & Sui, M. (2011) · InTech eBooks · doi:10.5772/21786 · Cited by 1

Endoplasmic Reticulum Stress and Autophagy in Cancer

Tan, M., Tan, H. K., & Muhammad, T. S. T. (2020) · Springer eBooks · doi:10.1007/978-3-030-30845-2_18 · Cited by 1

Discovery and Chemical Development of Amcenestrant: An Oral Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer

El‐Ahmad, Y., Croq, V., Wehrey, C., et al. (2022) · ACS symposium series · doi:10.1021/bk-2022-1423.ch007 · Cited by 1

Ligand- and Structure-Based Drug Design of Non-Steroidal Aromatase Inhibitors (NSAIs) in Breast Cancer

Jha, T., Adhikari, N., Halder, A. K., & Saha, A. (2016) · IGI Global eBooks · doi:10.4018/978-1-5225-0549-5.ch004 · Cited by 1

Opportunities for development of novel therapies targeting steroid hormone receptors

Bai, C., Flores, O. A., & Schmidt, A. (2007) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2.5.725 · Cited by 1

Introduction: The Rationale for the Development of Targeted Drugs in Cancer Therapy

Groner, B. (2007) · Springer eBooks · doi:10.1007/978-3-540-31209-3_1

Hormonal Therapy in Cancer

Maunglay, S., Cogburn, J., & Münster, P. N. (2010) · Springer eBooks · doi:10.1007/978-90-481-9704-0_9

Development of an automated multi-dimensional workflow and its applications in clinical proteomics

Kullolli, M. (2011) · doi:10.17760/d20000895

Dysregulation of microRNA expression in acquired endocrine-resistant breast cancer.

Manavalan, T. T. (2012) · doi:10.18297/etd/897

EFFECT OF ESTRADIOL, IMIPRAMINE AND FLUOXETINE ON BRAIN SEROTONIN LEVELS IN OVARIECTOMIZED-INDUCED OSTEOPOROTIC RATS

Zakaria, N. (2017) · ˜Al-œAzhar Journal of Pharmaceutical Sciences/Al-Azhar Journal of Pharmaceutical Sciences · doi:10.21608/ajps.2017.28413

Breast

Ross, D. S. (2019) · Springer eBooks · doi:10.1007/978-3-030-22922-1_8

Hormone Signaling

Weatherman, R. V. (2008) · Wiley eBooks · doi:10.1002/9780470048672.wecb229

Design, Docking, In silico ADME Prediction of Novel 2-substituted-5- hydroxy-1-(1-methyl-3-morpholinopropyl)-1H-indole-3-carboxamide Derivatives for Estrogen Receptor Alfa in AF-2 Domain for Effective Anticancer Treatment

Wagh, S. N., & Chatpalliwar, V. A. (2022) · Letters in Drug Design & Discovery · doi:10.2174/1570180819666220613091348

Design and Optimization of Oestrogen Receptor PROTACs Based on 4-HydroxytamoxifenPreprint

Riéra, A., Loren, G., Espuny, I., et al. (2022) · SSRN Electronic Journal · doi:10.2139/ssrn.4126049

Data from Extranuclear Coactivator Signaling Confers Insensitivity to Tamoxifen

Kumar, R., Zhang, H., Holm, C., Vadlamudi, R. K., Landberg, G., & Rayala, S. K. (2023) · doi:10.1158/1078-0432.c.6517384

Data from Extranuclear Coactivator Signaling Confers Insensitivity to Tamoxifen

Kumar, R., Zhang, H., Holm, C., Vadlamudi, R. K., Landberg, G., & Rayala, S. K. (2023) · doi:10.1158/1078-0432.c.6517384.v1

Potent phytoregulators from Pyrenacantha volubilis targeting ERα: a promising natural alternative for breast cancer therapy

Manoharan, M. A., Umapathy, S., & Beutline Malgija, M. (2025) · 3 Biotech · doi:10.1007/s13205-025-04315-4

Impact of ESRRG expression on proliferation and metastasis in laryngeal squamous cell carcinoma

Hu, Y., Zhou, C., & Shen, Z. (2025) · Annals of Medicine and Surgery · doi:10.1097/ms9.0000000000003715

Regio- and Stereoselective Synthesis of CF 3 -Containing 1,2- and 1,1-Diarylethenes. Switchable Reaction of β-Halo-β-(trifluoromethyl)styrenes with Boronic Acids

Muzalevskiy, V. M., Sizova, Z. A., Vasil’ev, A. A., & G., V. G. V. (2026) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.5c02697

Design and Synthesis of Novel 1,2,3-Triazole Derivatives as Non-Steroidal Aromatase Inhibitors for Estrogen-Responsive Breast Cancer

Mansour, A., Hassan, L., & Saeed, O. (2023) · Pharmaceutical Sciences and Drug Design · doi:10.51847/flor0ckeu2

Design, synthesis, and biological evaluation of selective estrogen receptor modulators (SERMs) as anticancer agents for ER-positive breast cancer

Saini, A., Mythri, C., Kalita, R., et al. (2026) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2026.118763

Real-world estrogen receptor alpha 1 (ESR1) testing patterns and results for ER+/HER2- metastatic breast cancer in the United States, 2018–2024

Meisel, J., Pham, T., Chen, C., Kris, A., & Roose, J. P. (2026) · Breast Cancer Research and Treatment · doi:10.1007/s10549-026-08060-x

Autophagy and Necroptosis in Cancer

Tan, M., Tan, H. K., Moad, A. I. H., & Muhammad, T. S. T. (2014) · Springer eBooks · doi:10.1007/978-3-662-44006-3_14

The effect of selective estrogen receptor modulator administration on the hypothalamic-pituitary-testicular axis in men with idiopathic oligozoospermia

Tsourdi, E. A., Kourtis, A., Farmakiotis, D., Katsikis, I., Salmas, M., & Panidis, D. (2008) · Fertility and Sterility · doi:10.1016/j.fertnstert.2008.06.002 · Cited by 25

A Novel Strategy to Improve Women’s Health: Selective Estrogen Receptor Modulators

Abderrahman, B., & Jordan, V. C. (2018) · Cancer drug discovery and develogment/Cancer drug discovery and development · doi:10.1007/978-3-319-99350-8_8 · Cited by 6

SERMs: current status and future trends

Morello, K. C. (2002) · Critical Reviews in Oncology/Hematology · doi:10.1016/s1040-8428(02)00022-7 · Cited by 76

Arzoxifene in postmenopausal women with normal or low bone mass

Bolognese, M. A., Krege, J. H., Utian, W. H., et al. (2009) · Bone · doi:10.1016/j.bone.2009.03.084

Selective Estrogen Receptor Modulators for Postmenopausal Osteoporosis

Gennari, L., Merlotti, D., Valleggi, F., Martini, G., & Nuti, R. (2007) · Drugs & Aging · doi:10.2165/00002512-200724050-00002 · Cited by 106