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. 2005 Mar;7(3):275-86.
doi: 10.1016/j.ccr.2005.02.009.

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

Kiranmai Gumireddy  1 , M V Ramana Reddy, Stephen C Cosenza, R Boominathan, Stacey J Baker, Nabisa Papathi, Jiandong Jiang, James Holland, E Premkumar Reddy
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Free article

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

Kiranmai Gumireddy et al. Cancer Cell. 2005 Mar.
Free article

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.

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