Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

doi:10.1038/nchembio.1859

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Article

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

Nature chemical biology - 1 Aug 2015

Grebien Florian, Vedadi Masoud, Getlik Matthäus, Giambruno Roberto, Grover Amit, Avellino Roberto, Skucha Anna, Vittori Sarah, Kuznetsova Ekaterina, Smil David, Barsyte-Lovejoy Dalia, Li Fengling, Poda Gennadiy, Schapira Matthieu, Wu Hong, Dong Aiping, Senisterra Guillermo, Stukalov Alexey, Huber Kilian V M, Schönegger Andreas, Marcellus Richard, Bilban Martin, Bock Christoph, Brown Peter J, Zuber Johannes, Bennett Keiryn L, Al-Awar Rima, Delwel Ruud, Nerlov Claus, Arrowsmith Cheryl H, Superti-Furga Giulio

Abstract excerpt

The CEBPA gene is mutated in 9% of patients with acute myeloid leukemia (AML). Selective expression of a short (30-kDa) CCAAT-enhancer binding protein-α (C/EBPα) translational isoform, termed p30, represents the most common type of CEBPA mutation in AML. The molecular mechanisms underlying p30-mediated transformation remain incompletely understood. We show that C/EBPα p30, but not the normal p42 isoform,...

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PMID: 26167872
DOI: 10.1038/nchembio.1859
PMCID: PMC4511833

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