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Targeting PKM2 in cancer therapeutics: mechanistic advances and translational opportunities

Lin Liu1, Junyi Wang1, Libo Liang1

  • 1Drug Dispending Department, The Third Hospital of Mianyang, Sichuan Mental Health Center, Mianyang, China.

Frontiers in Immunology
|October 31, 2025
PubMed

Insights

Pyruvate kinase M2 (PKM2) drives cancer progression by altering cell metabolism and signaling. This review explores PKM2

Area of Science:

  • Biochemistry
  • Oncology
  • Molecular Biology

Background:

  • M2-type pyruvate kinase (PKM2) is a key enzyme in aerobic glycolysis, often overexpressed in cancers.
  • PKM2's role extends beyond metabolism, influencing oncogenic processes like proliferation, invasion, and chemotherapy resistance.

Purpose of the Study:

  • To systematically review the biological functions of PKM2 in tumorigenesis.
  • To examine the signaling mechanisms underlying PKM2's oncogenic effects.
  • To summarize recent advances in PKM2-targeted cancer therapeutics.

Main Methods:

  • Literature review of studies on PKM2 function and targeting.
  • Systematic analysis of PKM2-mediated signaling pathways in various malignancies.
  • Overview of current and emerging PKM2-targeted therapeutic strategies.

Main Results:

  • PKM2 significantly contributes to tumor progression through both metabolic and non-metabolic functions.
  • PKM2 regulates multiple signaling pathways crucial for cancer cell survival and growth.
  • Targeting PKM2 presents a promising avenue for novel cancer therapies.

Conclusions:

  • PKM2 is a multifaceted oncoprotein with critical roles in cancer development and progression.
  • Understanding PKM2's complex roles is essential for developing effective targeted therapies.
  • Further research into PKM2 pathways may uncover new therapeutic strategies and drug targets.
Keywords:
M2-type pyruvate kinasePKM2-targeted therapeuticsaerobic glycolysisanti-cancersignaling networks

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