National Center for
4J52: Crystal Structure of Plk1 in Complex With a Pyrimidodiazepinone Inhibitor
Bioorg. Med. Chem. Lett. (2013) 23 p.3662-3666
Using structure-based drug design, we identified and optimized a novel series of pyrimidodiazepinone PLK1 inhibitors resulting in the selection of the development candidate TAK-960. TAK-960 is currently undergoing Phase I evaluation in adult patients with advanced solid malignancies.