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

Zheng Zhang1, Xiaolan Xing2, Peng Guan3

  • 1Department of Medicinal Chemistry, School of Pharmacy, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian, Shandong, 271016, PR China.

European Journal of Medicinal Chemistry
|March 25, 2021
PubMed

Insights

Polo-like kinases (PLKs) are crucial in cell division and cancer. Targeting PLKs, especially in combination with other agents, offers a potent strategy for enhanced cancer therapy and improved patient prognosis.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Polo-like kinases (PLKs) are vital regulators of cell cycle and proliferation.
  • Dysregulation of PLKs is implicated in various cancers, correlating with poor prognosis.
  • PLKs represent promising targets for novel anticancer drug development.

Purpose of the Study:

  • To review PLK family members and their roles in cancer.
  • To summarize recent advances in single-target PLK inhibitors and their structure-activity relationships (SARs).
  • To explore synergistic effects of dual-targeting strategies involving PLKs and other anti-cancer targets.

Main Methods:

  • Literature review of PLK inhibitors and dual-targeting agents.
  • Analysis of structure-activity relationships for PLK inhibitors.
  • Discussion of synergistic interactions between PLK inhibitors and other anticancer agents.

Main Results:

  • PLK inhibitors show promise as single-target anticancer agents.
  • Synergistic effects observed between PLK inhibitors and agents targeting BRD4, EEF2K, and Aurora kinases.
  • Emerging dual-target agents combining PLK inhibition with other mechanisms.

Conclusions:

  • Dual-targeting strategies involving PLKs offer enhanced efficacy over single-target therapies.
  • Further development of dual-target agents holds significant potential for improving cancer treatment outcomes.
Keywords:
InhibitorInhibitory activityPLKTarget

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