2. Academic Validation
  3. Targeting PIM kinases in cancer therapy: An update on pharmacological small-molecule inhibitors

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

  • Eur J Med Chem. 2024 Jan 15:264:116016. doi: 10.1016/j.ejmech.2023.116016.
Siwei Chen 1,  Yushang Yang 1,  Yong Yuan 2,  Bo Liu 3
Affiliations

Affiliations

  • 1 Department of Thoracic Surgery, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China.
  • 2 Department of Thoracic Surgery, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China. Electronic address: [email protected].
  • 3 Department of Thoracic Surgery, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China. Electronic address: [email protected].
PMID: 38071792 DOI: 10.1016/j.ejmech.2023.116016
Abstract

Pim kinases, a serine/threonine kinase family with three isoforms, has been well-known to participate in multiple physiological processes by phosphorylating various downstream targets. Accumulating evidence has recently unveiled that aberrant upregulation of Pim kinases (PIM1, PIM2, and PIM3) are closely associated with tumor cell proliferation, migration, survival, and even resistance. Inhibiting or silencing of Pim kinases has been reported have remarkable antitumor effects, such as anti-proliferation, pro-apoptosis and resensitivity, indicating the therapeutic potential of Pim kinases as potential druggable targets in many types of human cancers. More recently, several pharmacological small-molecule inhibitors have been preclinically and clinically evaluated and showed their therapeutic potential; however, none of them has been approved for clinical application so far. Thus, in this perspective, we focus on summarizing the oncogenic roles of Pim kinases, key signaling network, and pharmacological small-molecule inhibitors, which will provide a new clue on discovering more candidate antitumor drugs targeting Pim kinases in the future.

Keywords

Cancer therapy; PIM kinase; PIM1; PIM2; PIM3; Small-molecule inhibitor.

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