Xin-Ying Qian

Discovery of potent, selective, and orally bioavailable monocyclic pyridine-based PKMYT1 inhibitors that synergize with CHK1 inhibition in replication-stressed cancer cells.

PKMYT1 mediates the inhibitory phosphorylation of CDK1 and represents a promising synthetic lethal target in p53-deficient or CCNE1-amplified malignancies. A series of PKMYT1 inhibitors featuring a novel monocyclic pyridine core structure was discovered, exhibiting improved selectivity and enhanced drug-like properties...