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Targeting PIM kinases in cancer therapy: An update on pharmacological small-molecule inhibitors

Siwei Chen1, Yushang Yang1, Yong Yuan1

  • 1Department of Thoracic Surgery, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China.

European Journal of Medicinal Chemistry
|December 10, 2023
PubMed

Insights

PIM kinases (PIM1, PIM2, PIM3) drive cancer growth and resistance. Inhibiting these kinases shows significant antitumor potential, highlighting them as key targets for novel cancer therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • PIM kinases are serine/threonine kinases involved in numerous cellular processes.
  • Aberrant PIM kinase expression is linked to cancer proliferation, migration, survival, and drug resistance.

Purpose of the Study:

  • To summarize the oncogenic roles of PIM kinases.
  • To review the key signaling networks involving PIM kinases.
  • To discuss current pharmacological small-molecule inhibitors targeting PIM kinases.

Main Methods:

  • Literature review of PIM kinase functions in cancer.
  • Analysis of signaling pathways regulated by PIM kinases.
  • Overview of preclinical and clinical studies on PIM kinase inhibitors.

Main Results:

  • PIM kinases promote tumor progression and resistance.
  • Inhibition of PIM kinases demonstrates antitumor effects like anti-proliferation and apoptosis induction.
  • Several small-molecule inhibitors show therapeutic promise but lack clinical approval.

Conclusions:

  • PIM kinases are validated therapeutic targets for human cancers.
  • Further research into PIM kinase inhibitors is crucial for developing new anticancer drugs.
  • Understanding PIM kinase signaling networks can guide future drug discovery efforts.
Keywords:
Cancer therapyPIM kinasePIM1PIM2PIM3Small-molecule inhibitor

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