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Discovery of novel covalent selective estrogen receptor degraders against endocrine-resistant breast cancer

https://doi.org/10.1016/j.apsb.2023.05.005

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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

inferredcites →https://doi.org/10.1002/9783527623297.ch5openalex-snapshot

Estrogen Receptors as Therapeutic Targets in Breast Cancer

inferredcites →https://doi.org/10.1002/cmdc.201200048openalex-snapshot

Development of Selective Estrogen Receptor Modulator (SERM)‐Like Activity Through an Indirect Mechanism of Estrogen Receptor Antagonism: Defining the Binding Mode of 7‐Oxabicyclo[2.2.1]hept‐5‐ene Scaffold Core Ligands

inferredcites →https://doi.org/10.1002/cmdc.202000473openalex-snapshot

The Quest for Orally Available Selective Estrogen Receptor Degraders (SERDs)

inferredcites →https://doi.org/10.1016/j.breast.2014.01.016openalex-snapshot

The therapeutic role of fulvestrant in the management of patients with hormone receptor-positive breast cancer

inferredcites →https://doi.org/10.1016/j.chembiol.2021.03.005openalex-snapshot

The role of reversible and irreversible covalent chemistry in targeted protein degradation

inferredcites →https://doi.org/10.1016/j.clbc.2011.02.002openalex-snapshot

Fulvestrant Revisited: Efficacy and Safety of the 500-mg Dose

inferredcites →https://doi.org/10.1016/j.ejmech.2019.03.058openalex-snapshot

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

inferredcites →https://doi.org/10.1016/j.ejmech.2019.111605openalex-snapshot

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

inferredcites →https://doi.org/10.1016/j.ejmech.2020.112689openalex-snapshot

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

inferredcites →https://doi.org/10.1016/s0140-6736(16)32389-3openalex-snapshot

Fulvestrant 500 mg versus anastrozole 1 mg for hormone receptor-positive advanced breast cancer (FALCON): an international, randomised, double-blind, phase 3 trial

inferredcites →https://doi.org/10.1021/acs.jmedchem.0c00913openalex-snapshot

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

inferredcites →https://doi.org/10.1021/acs.jmedchem.2c00008openalex-snapshot

Discovery of Thieno[2,3-e]indazole Derivatives as Novel Oral Selective Estrogen Receptor Degraders with Highly Improved Antitumor Effect and Favorable Druggability

inferredcites →https://doi.org/10.1021/acs.jmedchem.2c00525openalex-snapshot

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

inferredcites →https://doi.org/10.1021/acs.jmedchem.5b00054openalex-snapshot

Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts

inferredcites →https://doi.org/10.1021/acs.jmedchem.5b00099openalex-snapshot

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

inferredcites →https://doi.org/10.1021/acs.jmedchem.5b00760openalex-snapshot

Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer

inferredcites →https://doi.org/10.1021/acs.jmedchem.8b00224openalex-snapshot

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

inferredcites →https://doi.org/10.1021/acs.jmedchem.8b01572openalex-snapshot

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

inferredcites →https://doi.org/10.1021/bi991176kopenalex-snapshot

Cysteine 530 of the Human Estrogen Receptor α Is the Main Covalent Attachment Site of 11β-(Aziridinylalkoxyphenyl)estradiols

inferredcites →https://doi.org/10.1021/jm0506773openalex-snapshot

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

inferredcites →https://doi.org/10.1021/jm200801hopenalex-snapshot

The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: Addressing the “Core Issue” in the Design of Estrogen Receptor Ligands

inferredcites →https://doi.org/10.1021/jm3008745openalex-snapshot

Discovery of a Potent and Isoform-Selective Targeted Covalent Inhibitor of the Lipid Kinase PI3Kα

inferredcites →https://doi.org/10.1038/nature09472openalex-snapshot

Quantitative reactivity profiling predicts functional cysteines in proteomes

inferredcites →https://doi.org/10.1038/nchembio.2236openalex-snapshot

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

inferredcites →https://doi.org/10.1038/nrd.2016.211openalex-snapshot

Induced protein degradation: an emerging drug discovery paradigm

inferredcites →https://doi.org/10.1038/nrd2372openalex-snapshot

Strategies for the discovery and development of therapies for metastatic breast cancer

inferredcites →https://doi.org/10.1038/nrd3410openalex-snapshot

The resurgence of covalent drugs

inferredcites →https://doi.org/10.1038/s41573-022-00542-zopenalex-snapshot

Advances in covalent drug discovery

inferredcites →https://doi.org/10.1039/c9cs00720bopenalex-snapshot

Advances in covalent kinase inhibitors

inferredcites →https://doi.org/10.1073/pnas.2101657118openalex-snapshot

Dual-mechanism estrogen receptor inhibitors

inferredcites →https://doi.org/10.1093/jnci/djr257openalex-snapshot

Incidence of Breast Cancer in the United States: Current and Future Trends

inferredcites →https://doi.org/10.1158/0008-5472.can-18-3634openalex-snapshot

Estrogen Receptor Covalent Antagonists: The Best Is Yet to Come

inferredcites →https://doi.org/10.1158/1535-7163.mct-21-0378openalex-snapshot

Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer

inferredcites →https://doi.org/10.1158/2159-8290.cd-17-1229openalex-snapshot

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

inferredcites →https://doi.org/10.1177/1087057113502673openalex-snapshot

High-Throughput Screening Assays for Estrogen Receptor by Using Coumestrol, a Natural Fluorescence Compound

inferredcites →https://doi.org/10.1200/jco.2021.39.15_suppl.1018openalex-snapshot

Phase I/II study of H3B-6545, a novel selective estrogen receptor covalent antagonist (SERCA), in estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer.

inferredcites →https://doi.org/10.2174/156802606776173483openalex-snapshot

Estrogen Receptors as Therapeutic Targets in Breast Cancer

inferredcites →https://doi.org/10.3322/caac.21590openalex-snapshot

Cancer statistics, 2020

inferredcites →https://doi.org/10.3389/fonc.2018.00227openalex-snapshot

Recent Advances in the Treatment of Breast Cancer

inferredcites →https://doi.org/10.3390/cells8020089openalex-snapshot

Metabolic Reprogramming in Breast Cancer and Its Therapeutic Implications

inferredcites →https://doi.org/10.3390/ijms22157812openalex-snapshot

Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective

inferredcites →https://doi.org/10.4155/fmc-2020-0236openalex-snapshot

10 Years Into the Resurgence of Covalent Drugs

inferredcites →https://doi.org/10.7554/elife.12792openalex-snapshot

Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation

inferredcites →https://doi.org/10.7554/elife.37161openalex-snapshot

The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

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inferred← citeshttps://doi.org/10.1002/ctd2.70195openalex-snapshot

Computational strategies to address therapeutic resistance in estrogen receptor‐positive breast cancer: A narrative review of molecular docking, molecular dynamics simulations, and emerging therapeutic targets

inferred← citeshttps://doi.org/10.1002/med.22101openalex-snapshot

Unleashing the Power of Covalent Drugs for Protein Degradation

inferred← citeshttps://doi.org/10.1016/bs.apcsb.2024.10.001openalex-snapshot

Leveraging nuclear receptor mediated transcriptional signaling for drug discovery: Historical insights and current advances

inferred← citeshttps://doi.org/10.1016/j.apsb.2025.04.030openalex-snapshot

Discovery of Yersinia LcrV as a novel biased agonist of formyl peptide receptor 1 to bi-directionally modulate intracellular kinases in triple-negative breast cancer

inferred← citeshttps://doi.org/10.1016/j.apsb.2025.10.031openalex-snapshot

DHL-11, a novel prieurianin-type limonoid isolated from Munronia henryi, targeting IMPDH2 to inhibit triple-negative breast cancer

inferred← citeshttps://doi.org/10.1016/j.apsb.2026.05.001openalex-snapshot

Targeting RSK2 reverses endocrine resistance in ER-positive breast cancer via inhibiting the c-Myc–ERBB4 signaling pathway

inferred← citeshttps://doi.org/10.1016/j.apsb.2026.07.050openalex-snapshot

Post CDK4/6 inhibitors: Novel targeted combinations based on SERDs in HR+/HER2– advanced breast cancer

inferred← citeshttps://doi.org/10.1016/j.bbagen.2025.130775openalex-snapshot

Change in selectivity of estrogen receptor alpha ligand-binding domain by mutations at residues H524/L525

inferred← citeshttps://doi.org/10.1016/j.bioorg.2023.106919openalex-snapshot

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

inferred← citeshttps://doi.org/10.1016/j.bioorg.2026.110129openalex-snapshot

A novel ERα-targeted hydrophobic tag degrader, overcomes tamoxifen resistance via unfolded protein response-induced apoptosis and homologous recombination repair inhibition in breast cancer

inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116184openalex-snapshot

Fluorescence theranostic PROTACs for real-time visualization of ERα degradation

inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116393openalex-snapshot

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

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A distinct zearalenone detoxification strategy mediated by cytochrome P450

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Discovery of D-Ring-Contracted Artemisinin as a Potent Hydrophobic Tag for Targeted Protein Degradation

inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5c00490openalex-snapshot

Rational Design of Methylene Blue–Raloxifene Conjugates for Efficient Breast Tumor Elimination Triggered by ERα Degradation

inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5c00495openalex-snapshot

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

inferred← citeshttps://doi.org/10.1021/acs.jmedchem.5c02812openalex-snapshot

Drug-Conjugated Tam-NHC-Gold(I) Complexes Overcome ESR1 Mutant Breast Cancer Resistance and Downregulate the RAMP3/CALCR Signaling Pathway

inferred← citeshttps://doi.org/10.1038/s41467-025-62288-7openalex-snapshot

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

inferred← citeshttps://doi.org/10.1177/17588359251344007openalex-snapshot

Vaginal health in breast cancer survivors: a practical clinical approach

inferred← citeshttps://doi.org/10.15212/amm-2024-0006openalex-snapshot

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

inferred← citeshttps://doi.org/10.20935/acadonco8139openalex-snapshot

Adjuvant endocrine therapy in high-risk HR-positive and HER2-negative early breast cancer

inferred← citeshttps://doi.org/10.21037/tbcr-24-16openalex-snapshot

A narrative review: research progress of adjuvant intensive endocrine therapy for early breast cancer

inferred← citeshttps://doi.org/10.3389/fonc.2025.1513225openalex-snapshot

Decoding estrogen receptor and GPER biology: structural insights and therapeutic advances in ERα−positive breast cancer

inferred← citeshttps://doi.org/10.3389/fonc.2026.1855542openalex-snapshot

Oral selective estrogen receptor degraders and biomarker-driven therapy in ER-positive breast cancer: mechanisms, clinical evidence, and future directions

inferred← citeshttps://doi.org/10.3390/molecules30020305openalex-snapshot

Pegylated NIR Fluorophore-Conjugated OBHSA Prodrug for ERα-Targeted Theranostics with Enhanced Imaging and Long-Term Retention

inferred← citeshttps://doi.org/10.62347/kivs3169openalex-snapshot

Receptor tyrosine kinases in breast cancer treatment: unraveling the potential

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