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All screens lead to polo-like kinase 1: A central node in cancer therapeutics and resistance

Norah Al-Souhibani1, Otilia Menyhart2, Maeva Dufies3

  • 1Research & Innovation, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia.

Pharmacological Research
|May 19, 2026
PubMed

Insights

Polo-like kinase 1 (PLK1) is a key target in cancer therapy. New inhibitors and combination strategies are needed to overcome modest clinical outcomes from monotherapy, improving cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Polo-like kinase 1 (PLK1) is a mitotic kinase frequently overexpressed in various cancers, correlating with poor prognosis and treatment resistance.
  • PLK1 is consistently identified as a critical therapeutic target in oncology through extensive research screens.

Purpose of the Study:

  • To review current understanding of PLK1 overexpression in cancer aggressiveness and therapy resistance.
  • To highlight the potential of next-generation PLK1 inhibitors and combination therapies.

Main Methods:

  • Literature review and synthesis of current research on PLK1 in cancer.
  • Analysis of preclinical and emerging clinical data for PLK1 inhibitors.

Main Results:

  • PLK1 inhibitors show promising preclinical anti-tumor activity but modest clinical outcomes as monotherapy.
  • PLK1's role extends to tumor progression, immune evasion, and the tumor microenvironment, suggesting broader therapeutic implications.
  • New-generation inhibitors like Onvansertib show synergistic potential with chemotherapy and immunotherapy.

Conclusions:

  • Refined patient stratification is crucial for effective PLK1 inhibition therapy.
  • Innovative combination regimens are necessary to fully exploit the therapeutic potential of targeting PLK1 in cancer treatment.
Keywords:
Alpelisib (PubChem ID 56649450)BAL0891(PubChem ID 37635936)BI 2536 (PubChem ID 11364421)Carboplatin (PubChem ID 10339178)Cisplatin (PubChem ID 5460033)Fluorouracil (5-FU) (PubChem ID 3385)Folinic acid (Leucovorin) (PubChem ID 135403648)GSK461364 (PubChem ID 15983966)Gemcitabine (PubChem ID 60750)Ipatasertib (PubChem ID 24788740)Irinotecan (PubChem ID 60838)Olaparib (PubChem ID 23725625)Onvansertib (PCM 075 / NMS P937) (PubChem ID 49792852)Paclitaxel (PubChem ID 36314)Plogosertib (PubChem ID 42640739)Polo-like kinase 1Rigosertib (PubChem ID 59603054)TAK-960 (PubChem ID 129626435)Thiostrepton (PubChem ID 16129666)Volasertib (BI 6727) (PubChem ID 10461508)

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