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Transcriptional kinases

Caught by a sticky drug

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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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Figure 1: THZ531 blocks optimal transcription elongation of DDR genes and super-enhancer-associated transcription factor genes in Jurkat cells.

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  1. Dalibor Blazek is at the Central European Institute of Technology (CEITEC), Masaryk University, Brno, Czech Republic.,

    Dalibor Blazek

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  1. Dalibor Blazek
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Correspondence to Dalibor Blazek.

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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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