PKMYT1

PKMYT1, or Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase, is a serine/threonine kinase also known as MYT1 or KIAA0070. It regulates cell cycle G2-to-M transition by phosphorylating CDK1 at Tyr15 and Thr14 residues, suppressing CDK1-cyclin B complex activity to maintain G2 checkpoint integrity upon DNA damage.
Aberrant PKMYT1 overexpression is linked to breast, lung, and colorectal cancers, driving uncontrolled proliferation and resistance to genotoxic therapies. Preclinical small-molecule inhibitors (e.g., MI-319) are under evaluation to abrogate G2 checkpoint, sensitize cancer cells to DNA-damaging agents, and overcome treatment resistance, representing a promising therapeutic direction.