The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma
Open accessAbstract
Many sarcomas and leukemias carry nonrandom chromosomal translocations encoding tumor-specific mutant fusion transcription factors that are essential to their molecular pathogenesis. Ewing's sarcoma family tumors (ESFTs) contain a characteristic t(11;22) translocation leading to expression of the oncogenic fusion protein EWS-FLI1. EWS-FLI1 is a disordered protein that precludes standard structure-based small-molecule inhibitor design. EWS-FLI1 binding to RNA helicase A (RHA) is important for its oncogenic function. We therefore used surface plasmon resonance screening to identify compounds that bind EWS-FLI1 and might block its interaction with RHA. YK-4-279, a derivative of the lead compound from the screen, blocks RHA binding to EWS-FLI1, induces apoptosis in ESFT cells and reduces the growth of ESFT orthotopic xenografts. These findings provide proof of principle that inhibiting the interaction of mutant cancer-specific transcription factors with the normal cellular binding partners required for their oncogenic activity provides a promising strategy for the development of uniquely effective, tumor-specific anticancer agents.
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The Amber biomolecular simulation programs
Case, D. A., Cheatham, T. E., Darden, T., Gohlke, H., Luo, R., Merz, K. M., Onufriev, A., Simmerling, C., Wang, B., & Woods, R. J. (2005) · Journal of Computational Chemistry · doi:10.1002/jcc.20290 · Cited by 9,535
The influence of drug-like concepts on decision-making in medicinal chemistry
Leeson, P. D., & Springthorpe, B. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2445 · Cited by 2,403
Gene fusion with an ETS DNA-binding domain caused by chromosome translocation in human tumours
Delattre, O., Zucman, J., Plougastel, B., Desmaze, C., Melot, T., Peter, M., Kovar, H., Joubert, I., de Jong, P., Rouleau, G., et al. (1992) · Nature · doi:10.1038/359162a0 · Cited by 1,907
The impact of translocations and gene fusions on cancer causation
Mitelman, F., Johansson, B., & Mertens, F. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2091 · Cited by 1,400
Microsatellites as EWS/FLI response elements in Ewing's sarcoma
Gangwal, K., Sankar, S., Hollenhorst, P. C., Kinsey, M., Haroldsen, S. C., Shah, A. A., Boucher, K. M., Watkins, W. S., Jorde, L. B., Graves, B. J., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0801073105 · Cited by 297 · cited 1×
“To further support YK-4-279 as a functional inhibitor of EWS-FLI1, we transfected COS7 cells with EWS-FLI1 and NR0B1 reporter-luciferase plasmid (containing EWS-FLI1 regulatory GGAA element”
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Pathological Unfoldomics of Uncontrolled Chaos: Intrinsically Disordered Proteins and Human Diseases
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Metadata
- Authors
- Erkizan, H. V., Kong, Y., Merchant, M., Schlottmann, S., Barber-Rotenberg, J. S., Yuan, L., Abaan, O. D., Chou, T.-H., Dakshanamurthy, S., Brown, M. L., Üren, A., & Toretsky, J. A.
- Venue
- Nature Medicine
- Published
- 2009-07
- Volume
- 15
- Issue
- 7
- Pages
- 750-756
- ISSN
- 1078-8956 (ISSN-L)
- 1546-170X
- OpenAlex
- W2007438323
- Cited by
- 452
- References
- 5
- FWCI
- 20.33
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. https://app.cochat.ai/papers/10.1038/nm.1983
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- Erkizan, H. V., Kong, Y., Merchant, M., Schlottmann, S., Barber-Rotenberg, J. S., Yuan, L., Abaan, O. D., Chou, T.-H., Dakshanamurthy, S., Brown, M. L., Üren, A., & Toretsky, J. A. (2009). A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. Nature Medicine. https://doi.org/10.1038/nm.1983
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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