2. Academic Validation
  3. Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1)

Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1)

  • Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083.
Zhe Nie 1,  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,  Robert Skene,  Hua Zou,  Xiaodong Cao,  Takashi Ichikawa
Affiliations

Affiliation

  • 1 Takeda California, 10410 Science Center Drive, San Diego, CA 92121, USA.
PMID: 23664874 DOI: 10.1016/j.bmcl.2013.02.083
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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