ArticleScientific reports2018
A Computational Assay of Estrogen Receptor α Antagonists Reveals the Key Common Structural Traits of Drugs Effectively Fighting Refractory Breast Cancers.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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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.
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Who cites it
31 citing papers in PubMed, 64 citations in OpenAlex.
- The natural L370F ERα variant confers endocrine resistance and sensitivity to ATRA in metastatic breast cancer cells.Cell communication and signaling : CCS · 2026Article
- Molecular Targets of Minor Cannabinoids in Breast Cancer: In Silico and In Vitro Studies.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Estrogen Receptor Alpha Mutations, Truncations, Heterodimers, and Therapies.Endocrinology · 2024Review
- The adverse outcome pathway for breast cancer: a knowledge management framework bridging biomedicine and toxicology.Discover oncology · 2023Review
- Exploring the Anticancer Activity of Tamoxifen-Based Metal Complexes Targeting Mitochondria.Journal of medicinal chemistry · 2023Article
- Switching from Aromatase Inhibitors to Dual Targeting Flavonoid-Based Compounds for Breast Cancer Treatment.Molecules (Basel, Switzerland) · 2023Article
- ESR1 activating mutations: From structure to clinical application.Biochimica et biophysica acta. Reviews on cancer · 2023Review
- Primary endocrine resistance of ER+ breast cancer with ESR1 mutations interrogated by droplet digital PCR.NPJ breast cancer · 2022Article
- ESR1 mutations and therapeutic resistance in metastatic breast cancer: progress and remaining challenges.British journal of cancer · 2022Review
- Forskolin Stimulates Estrogen Receptor (ER)International journal of endocrinology · 2022Article
- All-Atom Simulations Reveal a Key Interaction Network in the HLA-E/NKG2A/CD94 Immune Complex Fine-Tuned by the Nonameric Peptide.Journal of chemical information and modeling · 2021Article
- The effect of protein mutations on drug binding suggests ensuing personalised drug selection.Scientific reports · 2021Article
- Nonameric Peptide Orchestrates Signal Transduction in the Activating HLA-E/NKG2C/CD94 Immune Complex as Revealed by All-Atom Simulations.International journal of molecular sciences · 2021Article
- Estrogen-Like Effect of Mitotane Explained by Its Agonist Activity on Estrogen Receptor-α.Biomedicines · 2021Article
- New insights on CRISPR/Cas9-based therapy for breast Cancer.Genes and environment : the official journal of the Japanese Environmental Mutagen Society · 2021Review
- ERpred: a web server for the prediction of subtype-specific estrogen receptor antagonists.PeerJ · 2021Article
- Currently Applied Molecular Assays for IdentifyingInternational journal of molecular sciences · 2020Review
- Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor.International journal of environmental research and public health · 2020Article
- Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors.ACS medicinal chemistry letters · 2020Article
- Decrypting the Information Exchange Pathways across the Spliceosome Machinery.Journal of the American Chemical Society · 2020Article
Corrections and comments
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Authors and funding
8 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Somatic mutations of the Estrogen Receptor α (ERα) occur with an up to 40% incidence in ER sensitive breast cancer (BC) patients undergoing prolonged endocrine treatments. These polymorphisms are implicated in acquired resistance, disease relapse, and increased mortality rates, hence representing a current major clinical challenge. Here, multi-microseconds (12.5 µs) molecular dynamics simulations revealed that recurrent ERα polymorphisms (i. e. L536Q, Y537S, Y537N, D538G) (mERα) are constitutively active in their apo form and that they prompt the selection of an agonist (active)-like conformation even upon antagonists binding. Interestingly, our simulations rationalize, for the first time, the efficacy profile of (pre)clinically used Selective Estrogen Receptor Modulators/Downregulators (SERMs/SERDs) against these variants, enlightening, at atomistic level of detail, the key common structural traits needed by drugs able to effectively fight refractory BC types. This knowledge represents a key advancement for mechanism-based therapeutics targeting resistant ERα isoforms, potentially allowing the community to move a step closer to 'precision medicine' calibrated on patients' genetic profiles and disease progression.
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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.