ArticlePloS one2014
A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 60 citations in OpenAlex.
- Novel Biomarkers for Lymph Node Metastasis and Prognosis of Bladder Cancer by Bioinformatics Analysis.ACS omega · 2025Article
- Oncogenic Fusions HarboringCancers · 2025Review
- The Role of Pea3 Transcription Factor Subfamily in the Nervous System.Molecular neurobiology · 2025Review
- YK-4-279 Induces Osteosarcoma Cell Cycle Arrest, DNA Damage Response, and Apoptosis by Regulating the MAPK Cascade.Drug design, development and therapy · 2025Article
- FLI1 promotes IFN-γ-induced kynurenine production to impair anti-tumor immunity.Nature communications · 2024Article
- The DNA/RNA helicase DHX9 orchestrates the KDM2B-mediated transcriptional regulation of YAP1 in Ewing sarcoma.Oncogene · 2024Article
- Poly(ADP-ribose) Polyremase-1 (PARP-1) Inhibition: A Promising Therapeutic Strategy for ETS-Expressing Tumours.International journal of molecular sciences · 2023Review
- TK216 targets microtubules in Ewing sarcoma cells.Cell chemical biology · 2022Article
- The DNA/RNA helicase DHX9 contributes to the transcriptional program of the androgen receptor in prostate cancer.Journal of experimental & clinical cancer research : CR · 2022Article
- Novel Targeted Therapeutic Strategies for Ewing Sarcoma.Cancers · 2022Review
- ETS factors in prostate cancer.Cancer letters · 2022Review
- YK-4-279 Attenuates Progression of Pre-Existing Pigmented Lesions to Nodular Melanoma in a Mouse Model.Cancers · 2021Article
- FK506 binding protein 10: a key actor of collagen crosslinking in clear cell renal cell carcinoma.Aging · 2021Article
- Targeting Pan-ETS Factors Inhibits Melanoma Progression.Cancer research · 2021Article
- Article
- The ETS Inhibitor YK-4-279 Suppresses Thyroid Cancer Progression Independent ofFrontiers in oncology · 2021Article
- Glucose-Regulated Protein 94 Mediates the Proliferation and Metastasis through the Regulation of ETV1 and MAPK Pathway in Colorectal Cancer.International journal of medical sciences · 2021Article
- Androgen-Driven Fusion Genes and Chimeric Transcripts in Prostate Cancer.Frontiers in cell and developmental biology · 2021Review
- p53 Loss Mediates Hypersensitivity to ETS Transcription Factor Inhibition Based on PARylation-Mediated Cell Death Induction.Cancers · 2020Article
- 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
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Authors and funding
14 authors at 3 institutions in 1 country.
Funding
Abstract
backgroundThe erythroblastosis virus E26 transforming sequences (ETS) family of transcription factors consists of a highly conserved group of genes that play important roles in cellular proliferation, differentiation, migration and invasion. Chromosomal translocations fusing ETS factors to promoters of androgen responsive genes have been found in prostate cancers, including the most clinically aggressive forms. ERG and ETV1 are the most commonly translocated ETS proteins. Over-expression of these proteins in prostate cancer cells results in a more invasive phenotype. Inhibition of ETS activity by small molecule inhibitors may provide a novel method for the treatment of prostate cancer. METHODS AND
findingsWe recently demonstrated that the small molecule YK-4-279 inhibits biological activity of ETV1 in fusion-positive prostate cancer cells leading to decreased motility and invasion in-vitro. Here, we present data from an in-vivo mouse xenograft model. SCID-beige mice were subcutaneously implanted with fusion-positive LNCaP-luc-M6 and fusion-negative PC-3M-luc-C6 tumors. Animals were treated with YK-4-279, and its effects on primary tumor growth and lung metastasis were evaluated. YK-4-279 treatment resulted in decreased growth of the primary tumor only in LNCaP-luc-M6 cohort. When primary tumors were grown to comparable sizes, YK-4-279 inhibited tumor metastasis to the lungs. Expression of ETV1 target genes MMP7, FKBP10 and GLYATL2 were reduced in YK-4-279 treated animals. ETS fusion-negative PC-3M-luc-C6 xenografts were unresponsive to the compound. Furthermore, YK-4-279 is a chiral molecule that exists as a racemic mixture of R and S enantiomers. We established that (S)-YK-4-279 is the active enantiomer in prostate cancer cells.
conclusionOur results demonstrate that YK-4-279 is a potent inhibitor of ETV1 and inhibits both the primary tumor growth and metastasis of fusion positive prostate cancer xenografts. Therefore, YK-4-279 or similar compounds may be evaluated as a potential therapeutic tool for treatment of human prostate cancer at different stages.
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