The DOI matches its Crossref record; 43 of the 43 references it cites were found in a registry or an index.
Drugging MYCN through an Allosteric Transition in Aurora Kinase A
Open accessAbstract
Summary MYC proteins are major drivers of cancer, yet are considered undruggable, as their DNA binding domains are composed of two extended alpha helices with no apparent surfaces for small molecule binding. Proteolytic degradation of MYCN protein is regulated in part by a kinase-independent function of Aurora A. We describe a class of inhibitors that disrupts the native conformation of Aurora A, and drives degradation of MYCN protein across MYCN-driven cancers. Comparison of co-crystal structures with structure-activity relationships across multiple inhibitors and chemotypes, coupled with mechanistic studies and biochemical assays, delineates an Aurora A conformation-specific effect on proteolytic degradation of MYCN, rather than simple nanomolar-level inhibition of Aurora A kinase activity.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
1 retracted
BRCA1 Phosphorylation by Aurora-A in the Regulation of G2 to M Transition
Ouchi, M., Fujiuchi, N., Sasai, K., Katayama, H., Minamishima, Y. A., Ongusaha, P. P., Deng, C., Sen, S., Lee, S. W., & Ouchi, T. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m311780200 · Cited by 199
RetractedFeatures and development of Coot
Emsley, P., Lohkamp, B., Scott, W. G., & Cowtan, K. (2010) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444910007493 · Cited by 29,915
PHENIX : a comprehensive Python-based system for macromolecular structure solution
Adams, P. D., Afonine, P. V., Bunkóczi, G., Chen, V. B., Davis, I. W., Echols, N., Headd, J. J., Hung, L.-W., Kapral, G. J., Grosse-Kunstleve, R. W., et al. (2010) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444909052925 · Cited by 23,716
Selective inhibition of BET bromodomains
Filippakopoulos, P., Qi, J., Picaud, S., Shen, Y., Smith, W. B., Fedorov, O., Morse, E. M., Keates, T., Hickman, T. T., Felletar, I., et al. (2010) · Nature · doi:10.1038/nature09504 · Cited by 4,262
BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc
Delmore, J. E., Issa, G. C., Lemieux, M. E., Rahl, P. B., Shi, J., Jacobs, H. M., Kastritis, E., Gilpatrick, T., Paranal, R. M., Qi, J., et al. (2011) · Cell · doi:10.1016/j.cell.2011.08.017 · Cited by 2,813
Systematic identification of genomic markers of drug sensitivity in cancer cells
Garnett, M. J., Edelman, E. J., Heidorn, S. J., Greenman, C. D., Dastur, A., Lau, K. W., Greninger, P., Thompson, I. R., Luo, X., Soares, J., et al. (2012) · Nature · doi:10.1038/nature11005 · Cited by 2,456
Self-citationTranscriptional Amplification in Tumor Cells with Elevated c-Myc
Lin, C. Y., Lovén, J., Rahl, P. B., Paranal, R. M., Burge, C. B., Bradner, J. E., Lee, T. I., & Young, R. A. (2012) · Cell · doi:10.1016/j.cell.2012.08.026 · Cited by 1,513
Targeting MYC dependence in cancer by inhibiting BET bromodomains
Mertz, J. A., Conery, A. R., Bryant, B. M., Sandy, P., Balasubramanian, S., Mele, D. A., Bergeron, L., & Sims, R. J. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1108190108 · Cited by 1,110
c-Myc Is a Universal Amplifier of Expressed Genes in Lymphocytes and Embryonic Stem Cells
Nie, Z., Hu, G., Wei, G., Cui, K., Yamane, A., Resch, W., Wang, R., Green, D. R., Tessarollo, L., Casellas, R., et al. (2012) · Cell · doi:10.1016/j.cell.2012.08.033 · Cited by 1,075
Harrington, E. A., Bebbington, D., Moore, J., Rasmussen, R. K., Ajose-Adeogun, A. O., Nakayama, T., Graham, J. A., Demur, C., Hercend, T., Diu-Hercend, A., et al. (2004) · Nature Medicine · doi:10.1038/nm1003 · Cited by 965
Cited by
Drugging the ‘undruggable’ cancer targets
Dang, C. V., Reddy, E. P., Shokat, K. M., & Soucek, L. (2017) · Nature Reviews Cancer · doi:10.1038/nrc.2017.36 · Cited by 927
“In collaboration with my colleague William Weiss’s lab we carried out a targeted screen of AURKA inhibitors in search of amphosteric inhibitors of MYC 15 .”
Self-citationCellular plasticity and the neuroendocrine phenotype in prostate cancer
Davies, A. H., Beltran, H., & Zoubeidi, A. (2018) · Nature Reviews Urology · doi:10.1038/nrurol.2018.22 · Cited by 431
Glycolytic Metabolism Plays a Functional Role in Regulating Human Pluripotent Stem Cell State
Gu, W., Gaeta, X., Sahakyan, A., Chan, A. B., Hong, C. S., Kim, R., Braas, D., Plath, K., Lowry, W. E., & Christofk, H. R. (2016) · Cell Stem Cell · doi:10.1016/j.stem.2016.08.008 · Cited by 283
Hill, R. M., Kuijper, S., Lindsey, J. C., Petrie, K., Schwalbe, E. C., Barker, K., Boult, J. K. R., Williamson, D., Ahmad, Z., Hallsworth, A., et al. (2015) · Cancer Cell · doi:10.1016/j.ccell.2014.11.002 · Cited by 210
Self-citationCarabet, L. A., Rennie, P. S., & Cherkasov, A. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms20010120 · Cited by 172
Metadata
- Authors
- Gustafson, W. C., Meyerowitz, J. G., Nekritz, E. A., Chen, J., Benes, C., Charron, E., Simonds, E. F., Seeger, R., Matthay, K. K., Hertz, N. T., Eilers, M., Shokat, K. M., & Weiss, W. A.
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2014-09
- Volume
- 26
- Issue
- 3
- Pages
- 414-427
- ISSN
- 1535-6108 (ISSN-L)
- OpenAlex
- W1974771871
- Cited by
- 278
- References
- 43
- FWCI
- 10.45
- Type
- journal article
- Language
- en
- Open access
- bronze
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Drugging MYCN through an Allosteric Transition in Aurora Kinase A. https://app.cochat.ai/papers/10.1016/j.ccr.2014.07.015
- The paper
- Gustafson, W. C., Meyerowitz, J. G., Nekritz, E. A., Chen, J., Benes, C., Charron, E., Simonds, E. F., Seeger, R., Matthay, K. K., Hertz, N. T., Eilers, M., Shokat, K. M., & Weiss, W. A. (2014). Drugging MYCN through an Allosteric Transition in Aurora Kinase A. Cancer Cell. https://doi.org/10.1016/j.ccr.2014.07.015
Data sources
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).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
