The DOI matches its Crossref record; 177 of the 178 references it cites were found in a registry or an index.
Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer
Abstract
Estrogen receptor (ER) plays important roles in gene transcription and the proliferation of ER positive breast cancers. Selective modulation of ER has been a therapeutic target for this specific type of breast cancer for more than 30 years. Selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs) have been demonstrated to be effective therapeutic approaches for ER positive breast cancers. Unfortunately, 30-50% of ER positive tumors become resistant to SERM/AI treatment after 3-5 years. Fulvestrant, the only approved selective estrogen receptor degrader (SERD), is currently an important therapeutic approach for the treatment of endocrine-resistant breast cancers. The poor pharmacokinetic properties of fulvestrant have inspired the development of a new generation of oral SERDs to overcome drug resistance. In this review, we describe recent advances in ERα structure, functions, and mechanisms of endocrine resistance and summarize the development of oral SERDs in both academic and industrial areas.
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“Fulvestrant is a standard therapeutic option for endocrine-resistant or advanced metastatic ER+ breast cancer59,60.”
From Harnessing artificial intelligence to identify Bufalin as a molecular glue degrader of estrogen receptor alpha (2025) · cites this paper as [60]
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Lu, Y., Liu, L., Liang, Z., Schroder, W. A., Wen, Z., Zheng, T., Niu, B., Xie, C., Zhang, H., Min, J., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02812
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BindingDB Entry 50019323: Discovery of
BindingDB (2024) · UC San Diego · doi:10.7270/q2sx6jkk
BindingDB (2023) · UC San Diego · doi:10.7270/q2k0788f
Metadata
- Authors
- Lu, Y., & Liu, W.
- Affiliations
- Nanjing University of Chinese Medicine (CN)
- Corresponding author
- Lu, Yunlong
- Liu, Wukun
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2020-11-02
- Volume
- 63
- Issue
- 24
- Pages
- 15094-15114
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W3094721087
- Cited by
- 119
- References
- 178
- Citations by year
- 2026: 20 · 2025: 22 · 2024: 29 · 2023: 29 · 2022: 12 · 2021: 7
- FWCI
- 7.46
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Jiangsu Provincial Department of Education
- State Key Laboratory of Natural Medicines (SKLNMKF201712, SKLNMKF201808)
- Six Talent Peaks Project in Jiangsu Province (SWYY-069)
- National Natural Science Foundation of China (81703337)
- Priority Academic Program Development of Jiangsu Higher Education Institutions
- State Key Laboratory of Coordination Chemistry, Nanjing University
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Health Sciences › Medicine › Oncology › Advanced Breast Cancer Therapies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
- Keywords
- selective estrogen receptor degrader, estrogen receptor-positive breast cancer, endocrine therapy resistance, fulvestrant, aromatase inhibitors, selective estrogen receptor modulators, drug resistance mechanisms
- MeSH terms
- Fulvestrant, Breast Neoplasms, Clinical Trials as Topic, Female, Humans, Steroids, Structure-Activity Relationship, Signal Transduction, Drug Resistance, Neoplasm, Selective Estrogen Receptor Modulators, Aromatase Inhibitors, Estrogen Receptor alpha
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