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首页> 外文期刊>Cancer Cell >ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent.
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ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent.

机译：P0191的非ATP竞争性小分子抑制剂ON01910是有效的抗癌药。

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摘要

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.
机译：在许多人类肿瘤中都报道了polo样激酶1（Plk1）的表达升高，抑制Plk1活性导致其有丝分裂停滞和凋亡。在这里，我们描述了Plk1活性的小分子抑制剂ON01910的概况，它可诱导肿瘤细胞的有丝分裂停滞，其特征是纺锤体异常导致其凋亡。该化合物不具有ATP竞争性，但竞争该酶的底物结合位点。在体内，该化合物不表现出血液毒性，肝损伤或神经毒性，并且在多种异种移植裸鼠模型中是有效的肿瘤生长抑制剂。 ON01910与几种化学治疗剂表现出强大的协同作用，常常诱导肿瘤完全消退。

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