Literature DB >> 23664874

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

Zhe Nie1, 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.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23664874     DOI： 10.1016/j.bmcl.2013.02.083

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  13 in total

1.  Molecular modeling and structure-based drug discovery approach reveals protein kinases as off-targets for novel anticancer drug RH1.

Authors:  Pramodkumar P Gupta; Virupaksha A Bastikar; Dalius Kuciauskas; Shanker Lal Kothari; Jonas Cicenas; Mindaugas Valius
Journal:  Med Oncol       Date:  2017-09-06       Impact factor: 3.064

Review 2.  The accumulation of DNA repair defects is the molecular origin of carcinogenesis.

Authors:  Hyuk-Jin Cha; Hyungshin Yim
Journal:  Tumour Biol       Date:  2013-08-02

Review 3.  Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition.

Authors:  Brendan Frett; Robert V Brown; Mingliang Ma; Wenhao Hu; Haiyong Han; Hong-yu Li
Journal:  J Med Chem       Date:  2014-02-25       Impact factor: 7.446

Review 4.  Plk1 Inhibitors in Cancer Therapy: From Laboratory to Clinics.

Authors:  Rosie Elizabeth Ann Gutteridge; Mary Ann Ndiaye; Xiaoqi Liu; Nihal Ahmad
Journal:  Mol Cancer Ther       Date:  2016-06-21       Impact factor: 6.261

5.  Inhibition of polo like kinase 1 in sarcomas induces apoptosis that is dependent on Mcl-1 suppression.

Authors:  Jayasree S Nair; Gary K Schwartz
Journal:  Cell Cycle       Date:  2015       Impact factor: 4.534

Review 6.  Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels.

Authors:  Timothy P Heffron
Journal:  Neuro Oncol       Date:  2018-02-19       Impact factor: 12.300

7.  Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells.

Authors:  Na-Na Wang; Zhi-Heng Li; He Zhao; Yan-Fang Tao; Li-Xiao Xu; Jun Lu; Lan Cao; Xiao-Juan Du; Li-Chao Sun; Wen-Li Zhao; Pei-Fang Xiao; Fang Fang; Guang-Hao Su; Yan-Hong Li; Gang Li; Yi-Ping Li; Yun-Yun Xu; Hui-Ting Zhou; Yi Wu; Mei-Fang Jin; Lin Liu; Jian Ni; Jian Wang; Shao-Yan Hu; Xue-Ming Zhu; Xing Feng; Jian Pan
Journal:  Int J Mol Sci       Date:  2015-01-07       Impact factor: 5.923

Review 8.  PLK1, A Potential Target for Cancer Therapy.

Authors:  Zhixian Liu; Qingrong Sun; Xiaosheng Wang
Journal:  Transl Oncol       Date:  2016-11-24       Impact factor: 4.243

9.  PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase.

Authors:  Minoru Inoue; Michio Yoshimura; Minoru Kobayashi; Akiyo Morinibu; Satoshi Itasaka; Masahiro Hiraoka; Hiroshi Harada
Journal:  Sci Rep       Date:  2015-10-27       Impact factor: 4.379

10.  The clinical and prognostic value of polo-like kinase 1 in lung squamous cell carcinoma patients: immunohistochemical analysis.

Authors:  Hefei Li; Haibo Wang; Zhenqing Sun; Qiang Guo; Hongyun Shi; Youchao Jia
Journal:  Biosci Rep       Date:  2017-07-19       Impact factor: 3.840
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