ReviewACS omega2021
From Pure Antagonists to Pure Degraders of the Estrogen Receptor: Evolving Strategies for the Same Target.
Review in ACS omega, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 34 citations in OpenAlex.
- Loss of luminal lineage drives resistance to next-generation ERα antagonists in pretreated ERNature communications · 2026Article
- Monovalent pseudo-natural products supercharge degradation of IDO1 by its native E3 KLHDC3.Nature chemistry · 2026Article
- Allosteric Induction of Estrogen Receptor Ligand Binding Domain Tetramerization by a Distinct Complete Estrogen Receptor Antagonist.ACS medicinal chemistry letters · 2026Article
- Caution over haste: why novel endocrine therapy in early lines should wait in Estrogen receptor positive human epidermal growth factor receptor 2 negative breast cancer.Breast cancer research : BCR · 2026Review
- PROteolysis TArgeting Chimera (PROTAC) Estrogen Receptor Degraders for Treatment of Estrogen Receptor-Positive Advanced Breast Cancer.Targeted oncology · 2025Review
- An Estrogen Receptor β Agonist with AR Antagonist Activity from a Modern AsymmetricACS medicinal chemistry letters · 2025Article
- ERα dysfunction caused by ESR1 mutations and therapeutic pressure promotes lineage plasticity in ERNature cancer · 2025Article
- Current Status and Future Perspectives of Antibody-Drug Conjugates in Hormone Receptor-Positive Breast Cancer.Cancers · 2024Review
- Article
- Tailoring Potential Natural Compounds for the Treatment of Luminal Breast Cancer.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Novel Estrogen Receptor-Targeted Agents for Breast Cancer.Current treatment options in oncology · 2023Review
- Vanillin-Based Indolin-2-one Derivative Bearing a Pyridyl Moiety as a Promising Anti-Breast Cancer Agent via Anti-Estrogenic Activity.ACS omega · 2023Article
- Article
- An overview of PROTACs: a promising drug discovery paradigm.Molecular biomedicine · 2022Review
- Computational approaches to identify a novel binding site of BHPI on estrogen receptor alpha.Steroids · 2022Article
- AMEERA-5: a randomized, double-blind phase 3 study of amcenestrant plus palbociclibTherapeutic advances in medical oncology · 2022Article
- Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status.Drug design, development and therapy · 2022Review
- Fulvestrant-3-Boronic Acid (ZB716) Demonstrates Oral Bioavailability and Favorable Pharmacokinetic Profile in Preclinical ADME Studies.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Immunohistochemical Profiling of HER-2/neu, Steroid Hormone Receptors and KI-67 Biomarkers in A Cohort of Nigerian Women with Breast Cancer.Journal of the West African College of SurgeonsArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Pure antiestrogens, or selective estrogen receptor degraders (SERDs), have proven to be effective in treating breast cancer that has progressed on tamoxifen and/or aromatase inhibitors. However, the only FDA-approved pure antiestrogen, fulvestrant, is limited in efficacy by its low bioavailability. The search for orally bioavailable SERDs has continued for nearly as long as the clinical history of the injection-only fulvestrant. Oral SERDs that have been developed and tested in patients ranged from nonsteroidal ER binders containing an acrylic acid or amino side chain to bifunctional proteolysis-targeting chimera (PROTAC) pure ER degraders. Structural evolution in the development of oral SERD molecules has been closely associated with quantifiable ER-degrading potency, as seen in the structural comparison analysis of acrylic acid and basic amino side-chain-bearing SERDs. Failure to improve on fulvestrant in the clinical trials by numerous acidic SERDs and early basic SERDs is blamed on tolerability and/or insufficient efficacy, which will likely be overcome by the new-generation basic SERD molecules and PROTAC ER degraders with improved oral bioavailability, low toxicity, and superior efficacy of receptor degradation.
Identifiers
What OpenQuestion holds
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.