| First Author | Christensen CL | Year | 2014 |
| Journal | Cancer Cell | Volume | 26 |
| Issue | 6 | Pages | 909-922 |
| PubMed ID | 25490451 | Mgi Jnum | J:217744 |
| Mgi Id | MGI:5615525 | Doi | 10.1016/j.ccell.2014.10.019 |
| Citation | Christensen CL, et al. (2014) Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell 26(6):909-22 |
| abstractText | Small cell lung cancer (SCLC) is an aggressive disease with high mortality, and 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, in particular to THZ1, a recently identified covalent inhibitor of cyclin-dependent kinase 7. We find that expression of super-enhancer-associated transcription factor genes, including MYC family proto-oncogenes and neuroendocrine lineage-specific factors, is 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. |
