ArticleOncotarget2017
Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer.
Article in Oncotarget, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 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
27 citing papers in PubMed, 45 citations in OpenAlex.
- In Vivo Prostate Cancer Modelling: From the Pre-Clinical to the Clinical Setting.Life (Basel, Switzerland) · 2026Review
- Article
- Oncogenic Fusions HarboringCancers · 2025Review
- The Role of Pea3 Transcription Factor Subfamily in the Nervous System.Molecular neurobiology · 2025Review
- Review
- N-terminal domain of androgen receptor is a major therapeutic barrier and potential pharmacological target for treating castration resistant prostate cancer: a comprehensive review.Frontiers in pharmacology · 2024Review
- The catalytic subunit of DNA-PK regulates transcription and splicing of AR in advanced prostate cancer.The Journal of clinical investigation · 2023Article
- Poly(ADP-ribose) Polyremase-1 (PARP-1) Inhibition: A Promising Therapeutic Strategy for ETS-Expressing Tumours.International journal of molecular sciences · 2023Review
- The roles of ETS transcription factors in liver fibrosis.Human cell · 2023Review
- Review
- Seminal exosomes - An important biological marker for various disorders and syndrome in human reproduction.Saudi journal of biological sciences · 2021Review
- Targeted therapy of human leukemia xenografts in immunodeficient zebrafish.Scientific reports · 2021Article
- The use of zebrafish model in prostate cancer therapeutic development and discovery.Cancer chemotherapy and pharmacology · 2021Review
- Androgen-Driven Fusion Genes and Chimeric Transcripts in Prostate Cancer.Frontiers in cell and developmental biology · 2021Review
- An inhibitor of endothelial ETS transcription factors promotes physiologic and therapeutic vessel regression.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Integrated Analysis of the ETS Family in Melanoma Reveals a Regulatory Role of ETV7 in the Immune Microenvironment.Frontiers in immunology · 2020Article
- Computer-Aided Discovery of Small Molecule Inhibitors of Thymocyte Selection-Associated High Mobility Group Box Protein (TOX) as Potential Therapeutics for Cutaneous T-Cell Lymphomas.Molecules (Basel, Switzerland) · 2019Article
- Capicua regulates neural stem cell proliferation and lineage specification through control of Ets factors.Nature communications · 2019Article
- Characterization of the ERG-regulated Kinome in Prostate Cancer Identifies TNIK as a Potential Therapeutic Target.Neoplasia (New York, N.Y.) · 2019Article
- A New Era of Prostate Cancer Precision Medicine.Frontiers in oncology · 2019Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
22 authors at 2 institutions in 1 country.
Funding
Abstract
Genomic alterations involving translocations of the ETS-related gene ERG occur in approximately half of prostate cancer cases. These alterations result in aberrant, androgen-regulated production of ERG protein variants that directly contribute to disease development and progression. This study describes the discovery and characterization of a new class of small molecule ERG antagonists identified through rational in silico methods. These antagonists are designed to sterically block DNA binding by the ETS domain of ERG and thereby disrupt transcriptional activity. We confirmed the direct binding of a lead compound, VPC-18005, with the ERG-ETS domain using biophysical approaches. We then demonstrated VPC-18005 reduced migration and invasion rates of ERG expressing prostate cancer cells, and reduced metastasis in a zebrafish xenograft model. These results demonstrate proof-of-principal that small molecule targeting of the ERG-ETS domain can suppress transcriptional activity and reverse transformed characteristics of prostate cancers aberrantly expressing ERG. Clinical advancement of the developed small molecule inhibitors may provide new therapeutic agents for use as alternatives to, or in combination with, current therapies for men with ERG-expressing metastatic castration-resistant prostate cancer.
Indexed as
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.