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Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1)
Authors:Zhe Nie  Victoria Feher  Srinivasa Natala  Christopher McBride  Andre Kiryanov  Benjamin Jones  Betty Lam  Yan Liu  Stephen Kaldor  Jeffrey Stafford  Kouki Hikami  Noriko Uchiyama  Tomohiro Kawamoto  Yuichi Hikichi  Shin-ichi Matsumoto  Nobuyuki Amano  Lilly Zhang  David Hosfield  Takashi Ichikawa
Affiliation:1. Takeda California, 10410 Science Center Drive, San Diego, CA 92121, USA;2. Takeda Pharmaceutical Company, Ltd, 2-26-1, Muraokahigashi, Fujisawa, Kanagawa 251-855, Japan
Abstract: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.
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