ArticleACS medicinal chemistry letters2018
New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons.
Article in ACS medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
25 citing papers in PubMed.
- Hydrophobic tagging: A promising paradigm for targeted protein degradation.Cell insight · 2026Review
- Camizestrant in Combination with Three Globally Approved CDK4/6 Inhibitors in Women with ER+, HER2- Advanced Breast Cancer: Results from SERENA-1.Clinical cancer research : an official journal of the American Association for Cancer Research · 2025Article
- Decoding estrogen receptor and GPER biology: structural insights and therapeutic advances in ERα-positive breast cancer.Frontiers in oncology · 2025Review
- New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives.Acta materia medica · 2024Article
- Complete elimination of estrogen receptor α by PROTAC estrogen receptor α degrader ERD-148 in breast cancer cells.Breast cancer research and treatment · 2024Article
- Advances in the mechanism of CDK4/6 inhibitor resistance in HR+/HER2- breast cancer.Therapeutic advances in medical oncology · 2024Review
- The G Protein-Coupled Estrogen Receptor (GPER): A Critical Therapeutic Target for Cancer.Cells · 2023Review
- Advances in Endocrine Therapy for Hormone Receptor-Positive Advanced Breast Cancer.Current oncology reports · 2023Review
- Protein-Targeted Degradation Agents Based on Natural Products.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Annulated carbamates are precursors for the ring contraction of the adamantane framework.RSC advances · 2022Article
- Overcoming Cancer Drug Resistance Utilizing PROTAC Technology.Frontiers in cell and developmental biology · 2022Review
- PROTAC: targeted drug strategy. Principles and limitations.Russian chemical bulletin = Izvestiia Akademii nauk. Seriia khimicheskaia · 2022Review
- Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta.Journal of chemical information and modeling · 2021Article
- Proteolysis-targeting chimeras and their implications in breast cancer.Exploration of targeted anti-tumor therapy · 2021Review
- Proteasomal and lysosomal degradation for specific and durable suppression of immunotherapeutic targets.Cancer biology & medicine · 2020Review
- Computer-Aided Ligand Discovery for Estrogen Receptor Alpha.International journal of molecular sciences · 2020Review
- Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.Journal of medicinal chemistry · 2020Review
- Towards accurate high-throughput ligand affinity prediction by exploiting structural ensembles, docking metrics and ligand similarity.Bioinformatics (Oxford, England) · 2020Article
- PROTACs- a game-changing technology.Expert opinion on drug discovery · 2019Review
- ESR1 mutations in breast cancer.Cancer · 2019Review
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
An effective endocrine therapy for breast cancer is to selectively and effectively degrade the estrogen receptor (ER). Up until now, there have been largely only two molecular scaffolds capable of doing this. In this study, we have developed new classes of scaffolds that possess selective estrogen receptor degrader (SERD) and ER antagonistic properties. These novel SERDs potently inhibit MCF-7 breast cancer cell proliferation and the expression of ER target genes, and their efficacy is comparable to Fulvestrant. Unlike Fulvestrant, the modular protein-targeted chimera (PROTAC)-type design of these novel SERDs should allow easy diversification into a library of analogs to further fine-tune their pharmacokinetic properties including oral availability. This work also expands the pool of currently available PROTAC-type scaffolds that could be beneficial for targeted degradation of various other therapeutically important proteins.
Identifiers
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.