A new study reports THZ531 as a covalent CDK12/CDK13 inhibitor affecting transcription. Application of the compound in cells decreases transcription elongation of DNA damage response genes and key super-enhancer-associated transcription factor genes, with important implications for targeted cancer therapy.
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References
Fuda, N.J., Ardehali, M.B. & Lis, J.T. Nature 461, 186–192 (2009).
Bartkowiak, B. et al. Genes Dev. 24, 2303–2316 (2010).
Greifenberg, A.K. et al. Cell Rep. 14, 320–331 (2016).
Blazek, D. et al. Genes Dev. 25, 2158–2172 (2011).
Zhang, T. et al. Nat. Chem. Biol. 12, 876–884 (2016).
Kwiatkowski, N. et al. Nature 511, 616–620 (2014).
Yu, M. et al. Science 350, 1383–1386 (2015).
Bajrami, I. et al. Cancer Res. 74, 287–297 (2014).
Cancer Genome Atlas Research Network. Nature 474, 609–615 (2011).
Mertins, P. et al. Nature 534, 55–62 (2016).
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Blazek, D. Caught by a sticky drug. Nat Chem Biol 12, 765–766 (2016). https://doi.org/10.1038/nchembio.2184
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DOI: https://doi.org/10.1038/nchembio.2184
