Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer In Vitro and In Vivo

Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries

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Histone H3K27ac separates active from poised enhancers and predicts developmental state

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PROTAC targeted protein degraders: the past is prologue

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Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation

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Breast cancer

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Structural basis of PROTAC cooperative recognition for selective protein degradation

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Activating ESR1 mutations in hormone-resistant metastatic breast cancer

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Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 100-month analysis of the ATAC trial

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PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future

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Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial

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Estrogen receptors alpha (ERα) and beta (ERβ): Subtype-selective ligands and clinical potential

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TT-seq maps the human transient transcriptome

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Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation

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Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

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D538G Mutation in Estrogen Receptor-α: A Novel Mechanism for Acquired Endocrine Resistance in Breast Cancer

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Structural insights into the mode of action of a pure antiestrogen.

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Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

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PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

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Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives

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Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

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Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer

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Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs

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PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery

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Design, synthesis and biological evaluation of nuclear receptor-degradation inducers

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Endocrine treatment in breast cancer: Cure, resistance and beyond

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Estrogen signaling: An emanating therapeutic target for breast cancer treatment

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Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer

Snyder, L. B., Flanagan, J. J., Qian, Y., Gough, S. M., Andreoli, M., Bookbinder, M., Cadelina, G., Bradley, J., Rousseau, E., Chandler, J., et al. (2021) · Cancer Research · doi:10.1158/1538-7445.am2021-44 · Cited by 126 · see citing works

Development of Stabilized Peptide-Based PROTACs against Estrogen Receptor α

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Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced Cancer Therapy

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Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

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Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer

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Mitotic Transcriptional Activation: Clearance of Actively Engaged Pol II via Transcriptional Elongation Control in Mitosis

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Estrogen Receptor β as a Pharmaceutical Target

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Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer

Tang, C. C., Li, C., Zhang, S., Hu, Z., Wu, J., Dong, C., Huang, J., & Zhou, H. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00099 · Cited by 113 · see citing works

Estrogen receptor mutations and functional consequences for breast cancer

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The race to develop oral SERDs and other novel estrogen receptor inhibitors: recent clinical trial results and impact on treatment options

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Synthesis and Evaluation of Estrogen Receptor Ligands with Bridged Oxabicyclic Cores Containing a Diarylethylene Motif: Estrogen Antagonists of Unusual Structure

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Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer

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Full antagonism of the estrogen receptor without a prototypical ligand side chain

Srinivasan, S., Nwachukwu, J. C., Bruno, N. E., Dharmarajan, V., Goswami, D., Kastrati, I., Novick, S. J., Nowak, J., Cavett, V. J., Zhou, H., et al. (2016) · Nature Chemical Biology · doi:10.1038/nchembio.2236 · Cited by 66 · see citing works

Structurally Novel Antiestrogens Elicit Differential Responses from Constitutively Active Mutant Estrogen Receptors in Breast Cancer Cells and Tumors

Zhao, Y., Laws, M. J., Guillen, V. S., Ziegler, Y., Min, J., Sharma, A., Kim, S. H., Chu, D. T. W., Park, B. H., Oesterreich, S., et al. (2017) · Cancer Research · doi:10.1158/0008-5472.can-17-1265 · Cited by 60 · see citing works

Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases

Luo, X., Archibeque, I., Dellamaggiore, K., Smither, K., Homann, O. R., Lipford, J. R., & Mohl, D. A. (2022) · iScience · doi:10.1016/j.isci.2022.103985 · Cited by 53 · see citing works

Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer

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Exploring the PROTAC degron candidates: OBHSA with different side chains as novel selective estrogen receptor degraders (SERDs)

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Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer

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Bicyclic core estrogens as full antagonists: synthesis, biological evaluation and structure–activity relationships of estrogen receptor ligands based on bridged oxabicyclic core arylsulfonamides

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Proteolytic Targeting Chimeras with Specificity for Plasma Membrane and Intracellular Estrogen Receptors

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Anticancer or carcinogenic? The role of estrogen receptor β in breast cancer progression

Shen, K., Yu, H., Xie, B., Meng, Q., Dong, C., Shen, K., & Zhou, H. (2023) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2023.108350 · Cited by 36 · see citing works

Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor α (ERα) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer

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A New Era in ER+ Breast Cancer: Best-in-Class Oral Selective Estrogen Receptor Degrader (SERD) Designed as an Endocrine Backbone Treatment

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Novel class of 7-Oxabicyclo[2.2.1]heptene sulfonamides with long alkyl chains displaying improved estrogen receptor α degradation activity

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Three-dimensional oxabicycloheptene sulfonate targets the homologous recombination and repair programmes through estrogen receptor α antagonism

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Second Oral SERD Shines in ER+ Breast Cancer

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Discovery of ERD-3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity

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Targeting the Undruggable: Recent Progress in PROTAC-Induced Transcription Factor Degradation

Jung, H., & Lee, Y. (2025) · Cancers · doi:10.3390/cancers17111871 · Cited by 39 · see citing works

Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer

Xin, L., Wang, C., Cheng, Y., Wang, H., Guo, X., Deng, X., Deng, X., Xie, B., Hu, H., Min, C., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00196 · Cited by 38 · see citing works

Discovery of ERD-12310A as an Exceptionally Potent and Orally Efficacious PROTAC Degrader of Estrogen Receptor α (ERα)

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PROTAC: Novel degradable approach for different targets to treat breast cancer

Wang, Z., Che, S., & Yu, Z. (2024) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2024.106793 · Cited by 25 · see citing works

Recent advances in dual PROTACs degrader strategies for disease treatment

Liu, J., Liu, Y., Tang, J., Gong, Q., Yan, G., Fan, H., Zhang, X., & Pu, C. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116901 · Cited by 25 · see citing works

Harnessing artificial intelligence to identify Bufalin as a molecular glue degrader of estrogen receptor alpha

Jiang, S., Liu, K., Jiang, T., Li, H., Wei, X., Wan, X., Zhong, C., Gong, R., Chen, Z., Zou, C., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-62288-7 · Cited by 23 · see citing works

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

Min, J., Liu, X., Peng, R., Chen, C.-C., Wang, W., & Guo, R. (2024) · Acta Materia Medica · doi:10.15212/amm-2024-0006 · Cited by 20 · see citing works

Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

Jin, Y., & Lee, Y. (2024) · ChemMedChem · doi:10.1002/cmdc.202400267 · Cited by 18 · see citing works

Applications of Bridgehead Heterocycles in Drug Design and Medicinal Chemistry

Martino, S. D., Amico, P., & Rosa, M. D. (2025) · Topics in Current Chemistry · doi:10.1007/s41061-025-00502-2 · Cited by 16 · see citing works

Fluorescence theranostic PROTACs for real-time visualization of ERα degradation

Wang, X., Xin, L., Deng, X., Dong, C., Hu, G., & Zhou, H. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116184 · Cited by 15 · see citing works

Optimization of small molecule degraders and antagonists for targeting estrogen receptor based on breast cancer: current status and future

Yao, J., Tao, Y., Hu, Z., Li, J., Xue, Z., Zhang, Y., & Lei, Y. (2023) · Frontiers in Pharmacology · doi:10.3389/fphar.2023.1225951 · Cited by 12 · see citing works

Intercepting the Downstream of the Estrogen Receptor Signaling Pathway: Discovery of a Potent and Efficient SRC-3 PROTAC Degrader for Overcoming Endocrine Resistance Breast Cancer

Liang, J., Wang, D., Wu, Y., Shi, J., Xie, B., Xiao, R., Ni, J., Wang, C., Dong, C., Shu, H., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00425 · Cited by 11 · see citing works

Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer.

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Next‐Generation Proteolysis‐Targeting Chimeras in Precision Oncology: Multifunctional Designs, Emerging Modalities, and Translational Prospects in Targeted Protein Degradation

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Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance

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Targeted Degradation of the Estrogen Receptor α through Unconventional Coactivator Binding Site (CBS)

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Selective steroid receptor modulators, degraders and PROTACs: Therapeutic strategies in management of endocrine-related cancers

Tripathi, A., Chhabra, A., Rizvi, S., & Tyagi, R. K. (2025) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2025.112569 · Cited by 4 · see citing works

Highly potent and selective degrader targeting ERα to improve the treatment outcomes of breast cancer

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Multitargeted protein degradation: Integrating small-molecule, biomacromolecular, and nano-PROTACs for paradigm shifts in drug discovery

Yang, J., Zhang, Y., Zhang, M., Xing, D., & Wang, C. (2025) · Materials Today Advances · doi:10.1016/j.mtadv.2025.100644 · Cited by 3 · see citing works

Insight into Structure-Activity Relationship of New Compounds for Breast Cancer Treatment

Li, L., & Zhang, Q. (2023) · Current Topics in Medicinal Chemistry · doi:10.2174/0115680266253686230921054429 · Cited by 2 · see citing works

Kill Two Birds with One Stone: An Efficient and Potent AR CBS-Targeted Degrader Reverses Breast Cancer Resistance via Concurrent AR Degradation and ERα Transcriptional Suppression

Wu, Y., Xie, B., Liang, J., Wei, D., Wang, Y., Yin, Y., Deng, X., Wang, C., Ni, J., Yang, L., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01926 · Cited by 1 · see citing works

Discovery of Effective Dual PROTAC Degraders with Synergistic Antitumor Activity for Overcoming Tamoxifen-Resistant Breast Cancer

Xin, L., Liu, J., Guo, X., Li, S., Guo, Z., Wang, H., Song, Z., Deng, X., Wang, C., Fang, P. H., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c01189 · Cited by 1 · see citing works

Current Scenario of Sulfonamide Hybrids with Anti-Breast Cancer Therapeutic Applications: I. Sulfonamide-Five-Membered Heterocycle Hybrids

Xu, Z., & Ma, M. (2024) · Russian Journal of General Chemistry · doi:10.1134/s1070363224050177 · Cited by 1 · see citing works

THERAPEUTIC TARGETING OF AKT: STATUS AND FUTURE OPPORTUNITIES

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Structural evolution progress of orally bioavailable selective estrogen receptor degraders

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Propofol overcome Tamoxifen resistance in breast cancer by modulating tumorogenesis, immune response and metabolismPreprint

Yin, R., Gao, J., Guo, C., & Liu, Y. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.04.15.589641

Hypoxia-activated prodrugs

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Protacs Targeting ERα in the Effective Management of Endocrinal Resistance Breast Cancer

Singh, A., Khan, R., Erachampatt, N. A., Bhatia, N., Monga, V., & Thareja, S. (2025) · Archiv der Pharmazie · doi:10.1002/ardp.70176

An Estrogen Receptor α-Targeted NIR-II Probe for Breast Tumor Imaging and Image-Guided Surgery

Xu, D., Wang, L., Tang, Z., Xu, M., Huang, M., Jiang, T., & Tang, C. Y. (2026) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.6c00017

Nucleoside-ATTEC Conjugates for Targeting Inhibition of HIV Replication and Infection

Liao, X., Zhang, K., Wang, C., Liu, M., Ren, J., & Qu, X. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02422

Targeting drug resistance in breast cancer: a dual-perspective landscape analysis of PROTACs from bench to bedside

Yang, Y., & Lin, Y. W. (2026) · Breast Cancer Research · doi:10.1186/s13058-026-02320-w

NCP07: A potent ERα CBS-targeted degrader with dual-action against ESR1 mutations in breast cancer

Liang, J., Wu, Y., Yang, L., Xu, B., Wang, D., Shu, H., Dong, C., Li, S., & Zhou, H. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.119113

A Novel Dual-Targeting PROTAC Overcomes Endocrine Resistance by Engaging Orthosteric and Allosteric Sites of Estrogen Receptor α

Wang, C., Xu, B., Xin, L., Guo, Z., Deng, X., Dong, C., Yang, J., & Zhou, H. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00521

Bufalin-Loaded Multifunctional Nanodrugs for Cancer Therapy: Mechanisms, Delivery Strategies, and Translational Perspectives

Yang, Y., Zeng, X., Hu, Y., Su, Y., Li, C., Lv, F., Zhao, K., & Hu, J. (2026) · Biomolecules · doi:10.3390/biom16091297

BindingDB Entry 50021214: Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer.

BindingDB (2025) · UC San Diego · doi:10.7270/q2xd1691

BindingDB Entry 50021781: Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer.

BindingDB (2025) · UC San Diego · doi:10.7270/q2g165gx

BindingDB Entry 50022865: Discovery of ERD-12310A as an Exceptionally Potent and Orally Efficacious PROTAC Degrader of Estrogen Receptor α (ERα).

BindingDB (2026) · UC San Diego · doi:10.7270/q2c2529g

BindingDB Entry 50019323: Discovery of

BindingDB (2024) · UC San Diego · doi:10.7270/q2sx6jkk

Novel 11β-substituted estradiol conjugates: Transition from ERα agonizts to effective PROTAC degraders

Luo, G., Li, X., Lin, X., Lu, X., Li, Z., & Xiang, H. (2022) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2022.106154 · Cited by 5 · see citing works

Novel 11β -Substituted Estradiol Conjugates: Transition from Erα Agonists to Potent Protac DegradersPreprint

Luo, G., Li, X., Lin, X., Lu, X., Li, Z., & Xiang, H. (2022) · SSRN Electronic Journal · doi:10.2139/ssrn.4025200

Protacs Targeting ERα in the Effective Management of Endocrinal Resistance Breast Cancer

Singh, A., Khan, R., Erachampatt, N. A., Bhatia, N., Monga, V., & Thareja, S. (2025) · Archiv der Pharmazie · doi:10.1002/ardp.70176

Discovery of ERD-1233 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader for the Treatment of ER+ Human Breast Cancer

Acharyya, R. K., Rej, R. K., Hu, B., Chen, Z., Wu, D., Lü, J., Metwally, H., McEachern, D., Wang, Y., Jiang, W., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01521 · Cited by 23 · see citing works

Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance

Lin, X., Xiang, H., & Luo, G. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112689 · Cited by 100 · see citing works