ArticleMolecular systems biology2016
Predictive features of ligand-specific signaling through the estrogen receptor.
Article in Molecular systems biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 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
28 citing papers in PubMed, 53 citations in OpenAlex.
- Identification and Validation of the ESR1 Y537S Mutant-Enriched Enhancer and Its Downstream Target IGFBP3.Cancer research communications · 2026Article
- Multicomplex Pharmacophore Modeling of Estrogen Receptors Suggests the Probable Repurposing of Procaterol as an Antiproliferative Agent Against Breast Cancer Cells.International journal of molecular sciences · 2026Article
- cPEPmatch Webserver: A comprehensive tool and database to aid rational design of cyclic peptides for drug discovery.Computational and structural biotechnology journal · 2024Article
- Dataset from a human-in-the-loop approach to identify functionally important protein residues from literature.Scientific data · 2024Article
- Ancient and modern mechanisms compete in progesterone receptor activation.RSC chemical biology · 2024Article
- Bacterial Lactonases ZenA with Noncanonical Structural Features Hydrolyze the Mycotoxin Zearalenone.ACS catalysis · 2024Article
- Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells.NPJ breast cancer · 2022Article
- Human Estrogen Receptor Alpha Antagonists, Part 3: 3-D Pharmacophore and 3-D QSAR Guided Brefeldin A Hit-to-Lead Optimization toward New Breast Cancer Suppressants.Molecules (Basel, Switzerland) · 2022Article
- Quality Control for Single Cell Imaging Analytics Using Endocrine Disruptor-Induced Changes in Estrogen Receptor Expression.Environmental health perspectives · 2022Article
- Dual-mechanism estrogen receptor inhibitors.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Chemical systems biology reveals mechanisms of glucocorticoid receptor signaling.Nature chemical biology · 2021Article
- Nonsteroidal ecdysone receptor agonists use a water channel for binding to the ecdysone receptor complex EcR/USP.Journal of pesticide science · 2021Article
- ESR1 Mutations Associated With Estrogen Insensitivity Syndrome Change Conformation of Ligand-Receptor Complex and Altered Transcriptome Profile.Endocrinology · 2020Article
- Estrogen-induced transcription at individual alleles is independent of receptor level and active conformation but can be modulated by coactivators activity.Nucleic acids research · 2020Article
- Discovery of novel oestrogen receptor α agonists and antagonists by screening a revisited privileged structure moiety for nuclear receptors.Scientific reports · 2019Article
- Activity assessment of small drug molecules in estrogen receptor using multilevel prediction model.IET systems biology · 2019Article
- Pocket similarity identifies selective estrogen receptor modulators as microtubule modulators at the taxane site.Nature communications · 2019Article
- Perfluorinated compounds binding to estrogen receptor of different species: a molecular dynamic modeling.Journal of molecular modeling · 2018Article
- Role for Growth Regulation by Estrogen in Breast Cancer 1 (GREB1) in Hormone-Dependent Cancers.International journal of molecular sciences · 2018Review
- Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance.Nature reviews. Cancer · 2018Review
Corrections and comments
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Authors and funding
16 authors at 6 institutions in 3 countries.
Funding
Abstract
Some estrogen receptor-α (ERα)-targeted breast cancer therapies such as tamoxifen have tissue-selective or cell-specific activities, while others have similar activities in different cell types. To identify biophysical determinants of cell-specific signaling and breast cancer cell proliferation, we synthesized 241 ERα ligands based on 19 chemical scaffolds, and compared ligand response using quantitative bioassays for canonical ERα activities and X-ray crystallography. Ligands that regulate the dynamics and stability of the coactivator-binding site in the C-terminal ligand-binding domain, called activation function-2 (AF-2), showed similar activity profiles in different cell types. Such ligands induced breast cancer cell proliferation in a manner that was predicted by the canonical recruitment of the coactivators NCOA1/2/3 and induction of the GREB1 proliferative gene. For some ligand series, a single inter-atomic distance in the ligand-binding domain predicted their proliferative effects. In contrast, the N-terminal coactivator-binding site, activation function-1 (AF-1), determined cell-specific signaling induced by ligands that used alternate mechanisms to control cell proliferation. Thus, incorporating systems structural analyses with quantitative chemical biology reveals how ligands can achieve distinct allosteric signaling outcomes through ERα.
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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.