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Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles

Li Chen1,2,3, Wuyu Mao1, Changyu Ren4

  • 1Department of Neurology, Joint Research Institution of Altitude Health and Institute of Respiratory Health and National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.

Journal of Medicinal Chemistry
|January 2, 2024
PubMed

Insights

Proviral integration sitea (PIM) kinases regulate cellular processes. Small-molecule inhibitors targeting PIM, like Uzanserti, are advancing in clinical trials for cancers such as diffuse large B-cell lymphoma.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Proviral integration sitea (PIM) kinases (PIM-1, PIM-2, PIM-3) are highly conserved serine/tyrosine kinases.
  • PIM kinases regulate critical cellular functions including transcription, translation, proliferation, apoptosis, and energy metabolism via phosphorylation.

Purpose of the Study:

  • To review the structural and biological characteristics of PIM kinases.
  • To summarize research progress on PIM small-molecule inhibitors in clinical trials.
  • To evaluate challenges and explore recent medicinal chemistry efforts in PIM inhibitor discovery.

Main Methods:

  • Literature review of PIM kinase research.
  • Analysis of ongoing clinical trials for PIM inhibitors.
  • Exploration of medicinal chemistry strategies for small-molecule inhibitor design.

Main Results:

  • Several PIM inhibitors are in clinical development, with Uzanserti (5) completing Phase I trials for relapsed diffuse large B-cell lymphoma.
  • Recent advancements focus on the design and discovery of novel small-molecule inhibitors targeting PIM kinases.

Conclusions:

  • PIM kinases represent a promising therapeutic target in oncology.
  • Continued medicinal chemistry efforts are crucial for overcoming challenges and advancing PIM inhibitor development for clinical application.

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