Targeting polo-like kinases: A promising therapeutic approac for cancer treatment

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131 Scopus citations


Polo-like kinases (Plks) are a family of serine-threonine kinases that regulate multiple intracellular processes including DNA replication, mitosis, and stress response. Plk1, the most well understood family member, regulates numerous stages of mitosis and is overexpressed in many cancers. Plk inhibitors are currently under clinical investigation, including phase III trials of volasertib, a Plk inhibitor, in acute myeloid leukemia and rigosertib, a dual inhibitor of Plk1/phosphoinositide 3-kinase signaling pathways, in myelodysplastic syndrome. Other Plk inhibitors, including the Plk1 inhibitors GSK461364A, TKM-080301, GW843682, purpurogallin, and poloxin and the Plk4 inhibitor CFI-400945 fumarate, are in earlier clinical development. This review discusses the biologic roles of Plks in cell cycle progression and cancer, and the mechanisms of action of Plk inhibitors currently in development as cancer therapies.

Original languageEnglish
Pages (from-to)185-195
Number of pages11
JournalTranslational Oncology
Issue number3
StatePublished - 2015

Bibliographical note

Funding Information:
Medical writing assistance, supported financially by Boehringer Ingelheim Pharmaceuticals, Inc, was provided by Katie McClendon of GeoMed, an Ashfield company, part of UDG Healthcare plc, during the preparation of this review. Boehringer Ingelheim was given the opportunity to review for factual accuracy only. This work was supported by the National Institutes of Health (R01CA157429), the American Cancer Society (RSG-13-073-01-CNE), and the National Science Foundation (1049693-MCB). The author declares no conflicts of interest.

Publisher Copyright:
© 2015 The Authors. Published by Elsevier Inc.

ASJC Scopus subject areas

  • Oncology
  • Cancer Research


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