National Center for
3PP1: Crystal Structure of the Human Mitogen-activated protein kinase kinase 1 (MEK 1) in complex with ligand and MgATP
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
Bioorg. Med. Chem. Lett. (2011) 21 p.1315-1319
A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for cancer treatment.