The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Small Molecule Inhibitors of Aurora-A Induce Proteasomal Degradation of N-Myc in Childhood Neuroblastoma
Open accessAbstract
Summary Amplification of MYCN is a driver mutation in a subset of human neuroendocrine tumors including neuroblastoma. No small molecules that target N-Myc, the protein encoded by MYCN, are clinically available. N-Myc forms a complex with the Aurora-A kinase, which protects N-Myc from proteasomal degradation. Although stabilization of N-Myc does not require the catalytic activity of Aurora-A, we show here that two Aurora-A inhibitors, MLN8054 and MLN8237, disrupt the Aurora-A/N-Myc complex and promote degradation of N-Myc mediated by the Fbxw7 ubiquitin ligase. Disruption of the Aurora-A/N-Myc complex inhibits N-Myc-dependent transcription, correlating with tumor regression and prolonged survival in a mouse model of MYCN-driven neuroblastoma. We conclude that Aurora-A is an accessible target that makes destabilization of N-Myc a viable therapeutic strategy.
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Subramanian, A., Tamayo, P., Mootha, V. K., Mukherjee, S., Ebert, B. L., Gillette, M. A., Paulovich, A., Pomeroy, S. L., Golub, T. R., Lander, E. S., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0506580102 · Cited by 53,625
Yeh, E., Cunningham, M., Arnold, H., Chasse, D., Monteith, T., Ivaldi, G., Hahn, W. C., Stukenberg, P. T., Shenolikar, S., Uchida, T., et al. (2004) · Nature Cell Biology · doi:10.1038/ncb1110 · Cited by 791
Prognostic Impact of Gene Expression–Based Classification for Neuroblastoma
Oberthuer, A., Hero, B., Berthold, F., Juraeva, D., Faldum, A., Kahlert, Y., Asgharzadeh, S., Seeger, R., Scaruffi, P., Tonini, G. P., et al. (2010) · Journal of Clinical Oncology · doi:10.1200/jco.2009.27.3367 · Cited by 135
Self-citation
Cited by
Advances in Risk Classification and Treatment Strategies for Neuroblastoma
Pinto, N. R., Applebaum, M. A., Volchenboum, S. L., Matthay, K. K., London, W. B., Ambros, P. F., Nakagawara, A., Berthold, F., Schleiermacher, G., Park, J. R., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2014.59.4648 · Cited by 911
Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
Du, R., Huang, C., Liu, K., Li, X., & Dong, Z. (2021) · Molecular Cancer · doi:10.1186/s12943-020-01305-3 · Cited by 586
N-Myc Induces an EZH2-Mediated Transcriptional Program Driving Neuroendocrine Prostate Cancer
Dardenne, E., Beltran, H., Benelli, M., Gayvert, K., Berger, A., Puca, L., Cyrta, J., Sboner, A., Noorzad, Z., MacDonald, T., et al. (2016) · Cancer Cell · doi:10.1016/j.ccell.2016.09.005 · Cited by 559
Self-citationAurora kinases: novel therapy targets in cancers
Tang, A., Gao, K., Chu, L., Zhang, R., Yang, J., & Zheng, J. (2017) · Oncotarget · doi:10.18632/oncotarget.14893 · Cited by 382
Tumor suppression by the Fbw7 ubiquitin ligase: mechanisms and opportunities
Davis, R. J., Welcker, M., & Clurman, B. E. (2014) · Cancer Cell · doi:10.1016/j.ccell.2014.09.013 · Cited by 343
Metadata
- Authors
- Brockmann, M., Poon, E., Berry, T., Carstensen, A., Deubzer, H. E., Rycak, L., Jamin, Y., Thway, K., Robinson, S. P., Roels, F., Witt, O., Fischer, M., Chesler, L., & Eilers, M.
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2013-07
- Volume
- 24
- Issue
- 1
- Pages
- 75-89
- ISSN
- 1535-6108 (ISSN-L)
- OpenAlex
- W1995474832
- Cited by
- 299
- References
- 3
- FWCI
- 13.87
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Brockmann, M., Poon, E., Berry, T., Carstensen, A., Deubzer, H. E., Rycak, L., Jamin, Y., Thway, K., Robinson, S. P., Roels, F., Witt, O., Fischer, M., Chesler, L., & Eilers, M. (2013). Small Molecule Inhibitors of Aurora-A Induce Proteasomal Degradation of N-Myc in Childhood Neuroblastoma. Cancer Cell. https://doi.org/10.1016/j.ccr.2013.05.005
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
