[HTML][HTML] LLY-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase SMYD2

H Nguyen, A Allali-Hassani, S Antonysamy… - Journal of Biological …, 2015 - ASBMB
SMYD2 is a lysine methyltransferase that catalyzes the monomethylation of several protein
substrates including p53. SMYD2 is overexpressed in a significant percentage of
esophageal squamous primary carcinomas, and that overexpression correlates with poor
patient survival. However, the mechanism (s) by which SMYD2 promotes oncogenesis is not
understood. A small molecule probe for SMYD2 would allow for the pharmacological
dissection of this biology. In this report, we disclose LLY-507, a cell-active, potent small …