Recent progress in agents targeting polo-like kinases: Promising therapeutic strategies

Polo-like kinases (PLKs) play important roles in regulating multiple aspects of cell cycle and cell proliferation. In many cancer types, PLK family members are often dysregulated, which can lead to uncontrolled cell proliferation and aberrant cell division and has been shown to associate with poor prognosis of cancers. The key roles of PLK kinases in cancers lead to an enhanced interest in them as promising targets for anticancer drug development. In consideration of PLK inhibitors and some other anticancer agents, such as BRD4, EEF2K and Aurora inhibitors, exert synergy effects in cancer cells, dualtargeting of PLK and other cancer-related targets is regarded as an rational and potent strategy to enhance the effectiveness of single-targeting therapy for cancer treatment. This review introduces the PLK family members at first and then focuses on the recent advances of single-target PLK inhibitors and summarizes the corresponding SARs of them. Moreover, we discuss the synergisms between PLK and other anti-tumor targets, and sum up the current dual-target agents based on them. (C) 2021 Elsevier Masson SAS. All rights reserved.

Automated summary

Polo-like kinases (PLKs) are important in regulating cell cycle and proliferation, and dysregulation in cancers can lead to uncontrolled proliferation and poor prognosis. Targeting PLKs along with other cancer-related targets is considered a rational and potent strategy to enhance therapy effectiveness in cancer treatment.