WEE1 kinase has been reported to be aberrantly expressed in melanomas, glioblastoma multiforme (GBMs), triple negative breast cancers (TNBCs) and prostate cancers. Dependence of various cancer cells on WEE1 signaling suggests that targeting epigenetic activity of WEE1 is a viable strategy for overcoming tumor proliferation.

We designed an assay that provides specific and quantitative measure of WEE1 epigenetic activity. Library screen identified a new class of scaffolds, that efficiently suppressed WEE1 epigenetic activity and have shown propensity to overcome WEE1 mediated cell cycle regulation. 

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Schematic outlining WEE1 epigenetic and non-epigenetic functions in cell cycle. WEE1 is emerging as a critical surveyor of chromatin integrity across the evolutionary landscape by regulating histone synthesis and the cell cycle. Importantly, it appears to couple DNA synthesis with histone synthesis due to its ability to prevent mitotic entry until DNA synthesis is completed and to switch off histone transcription at the end of S phase. These functions are likely to be critical for its ability to delay chromosome condensation and prevent aneuploidy.