Andrew Simon Cook

TL;DR: It is demonstrated that β-catenin is not necessary for embryonic stem cell identity or expansion, but its absence eliminates the self-renewal response to Gsk3 inhibition, which stabilizes the embryonic stem Cell state primarily by reducing repressive influence on the core pluripotency network.

TL;DR: The discovery and structure–activity relationship (SAR) of a novel, small-molecule chemical probe for BET family inhibition that was identified through the application of structure-based fragment assessment and optimization techniques has yielded a potent, selective compound with cell-based activity (PFI-1) that may further add to the understanding of BET family function within the bromodomains.

TL;DR: The optimization of the indole-based EZH2 inhibitor series led to the identification of CPI-1205, a highly potent and selective inhibitor of EZh2 that demonstrates robust antitumor effects in a Karpas-422 xenograft model when dosed at 160 mg/kg BID and is currently in Phase I clinical trials.

TL;DR: Structural and computational studies reveal that an internal hydrogen bond stabilizes the protein-bound conformation of the dihydroquinoxalinone series and inhibits binding of CREBBP to chromatin in U2OS cells.

TL;DR: Agents for modulating methyl modifying enzymes, compositions and uses of such enzymes are described in this article, along with their properties and their applications in the field of bioinformatics.