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Targeting Pim kinases for cancer treatment: opportunities and challenges

Bich Thuy Le1, Malika Kumarasiri, Julian R J Adams

  • 1Centre for Drug Discovery & Development, Sansom Institute for Health Research, & School of Pharmacy & Medical Sciences, University of South Australia, Adelaide, SA 5001, Australia.

Future Medicinal Chemistry
|January 14, 2015
PubMed

Insights

Pim kinases are crucial in cancer development and are promising drug targets. This review explores Pim kinase inhibitors, their binding modes, and future opportunities for anticancer drug development.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Pim oncogenes are frequently overexpressed in various hematological and solid cancers.
  • Pim kinases play a critical role in regulating signaling pathways essential for tumorigenesis and cancer cell development.
  • Their involvement in cancer makes Pim kinases attractive targets for therapeutic intervention.

Purpose of the Study:

  • To review the current understanding of Pim kinase structure and biology.
  • To provide insights into the binding mechanisms of existing Pim-1 inhibitors.
  • To highlight challenges and opportunities in developing novel Pim kinase inhibitors for cancer treatment.

Main Methods:

  • Literature review of studies on Pim kinase inhibitors.
  • Analysis of structural and biological data related to Pim kinases.
  • Examination of binding modes of prototypical Pim-1 inhibitors.

Main Results:

  • Pim kinases are key regulators in cancer signaling pathways.
  • Current inhibitors primarily target the ATP-binding pocket in an ATP-competitive manner.
  • Understanding binding modes is crucial for designing effective inhibitors.

Conclusions:

  • Pim kinases represent a significant target for anticancer drug development.
  • Further research into inhibitor design, considering structure-activity relationships, is warranted.
  • Addressing challenges in inhibitor development can lead to effective new cancer therapies.

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