The synthesis of RP-1664, a highly potent, selective and bioavailable PLK4 inhibitor for the potential treatment of cancer, was recently reported by Repare Therapeutics Inc.

Tyrosine kinases (TKs) typically show strong binding affinity with a wide spectrum of type-II inhibitors while serine/threonine kinases (STKs) usually bind more weakly which we suggest here is due to ...