The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.
Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor
Open accessAbstract
SUMMARY Small cell lung cancer (SCLC) is an aggressive disease with high mortality. The identification of effective pharmacological strategies to target SCLC biology represents an urgent need. Using a high-throughput cellular screen of a diverse chemical library we observe that SCLC is sensitive to transcription-targeting drugs, and in particular to THZ1, a recent identified covalent inhibitor of cyclin-dependent kinase 7 (CDK7). We find that expression of super-enhancer associated transcription factor genes including MYC family proto-oncogenes and neuroendocrine lineage-specific factors are highly vulnerability to THZ1 treatment. We propose that downregulation of these transcription factors contributes, in part, to SCLC sensitivity to transcriptional inhibitors and that THZ1 represents a prototype drug for tailored SCLC therapy.
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Molecular subtypes of small cell lung cancer: a synthesis of human and mouse model data
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Kinase inhibitors: the road ahead
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Metadata
- Authors
- Christensen, C. L., Kwiatkowski, N., Abraham, B. J., Carretero, J., Al-Shahrour, F., Zhang, T., Chipumuro, E., Herter-Sprie, G. S., Akbay, E. A., Altabef, A., Zhang, J., Shimamura, T., Capelletti, M., Reibel, J. B., Cavanaugh, J. D., Gao, P., Liu, Y., Michaelsen, S. R., Poulsen, H. S., Aref, A. R., Barbie, D. A., Bradner, J. E., George, R. E., Gray, N. S., Young, R. A., & Wong, K.-K.
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2014-12
- Volume
- 26
- Issue
- 6
- Pages
- 909-922
- ISSN
- 1535-6108 (ISSN-L)
- OpenAlex
- W2072684537
- Cited by
- 439
- References
- 7
- FWCI
- 12.35
- Type
- journal article
- Language
- en
- Open access
- bronze
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- The paper
- Christensen, C. L., Kwiatkowski, N., Abraham, B. J., Carretero, J., Al-Shahrour, F., Zhang, T., Chipumuro, E., Herter-Sprie, G. S., Akbay, E. A., Altabef, A., Zhang, J., Shimamura, T., Capelletti, M., Reibel, J. B., Cavanaugh, J. D., Gao, P., Liu, Y., Michaelsen, S. R., Poulsen, H. S., . . . Wong, K.-K. (2014). Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor. Cancer Cell. https://doi.org/10.1016/j.ccell.2014.10.019
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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