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Cancer Cell. 2005 Mar;7(3):275-86.

ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent.

Author information

  • 1Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 N. Broad Street, Philadelphia, Pennsylvania 19140, USA.

Erratum in

  • Cancer Cell. 2005 May;7(5):497. Boomi Nathan, R [corrected to Boominathan, R].

Abstract

Elevated expression of polo-like kinase1 (Plk1) has been reported in many human tumors, and inhibition of Plk1 activity results in their mitotic arrest and apoptosis. Here we describe the profile of ON01910, a small molecule inhibitor of Plk1 activity, which induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. This compound was not ATP-competitive, but competed for the substrate binding site of the enzyme. In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models. ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors.

PMID:
15766665
[PubMed - indexed for MEDLINE]
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