REVIEW article
Front. Immunol.
Sec. Cancer Immunity and Immunotherapy
Volume 16 - 2025 | doi: 10.3389/fimmu.2025.1649488
Targeting PKM2 in Cancer Therapeutics: Mechanistic Advances and Translational Opportunities
Provisionally accepted- The Third People's Hospital of Mianyang, Mianyang, China
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M2-type pyruvate kinase (PKM2) serves as the key rate-limiting enzyme in aerobic glycolysis within tumor cells, where its aberrantly high expression in numerous human malignancies facilitates tumor progression by enhancing glycolytic flux through diverse signaling pathways. Beyond its metabolic function, extensive studies have established PKM2 as a critical non-metabolic signaling regulator implicated in multiple oncogenic processes, including tumor proliferation, invasion, migration, immune evasion, and resistance to chemotherapy. The elucidation of PKM2-mediated oncogenic pathways has spurred the development of targeted therapeutic strategies, positioning PKM2 as a promising target in cancer therapy. However, comprehensive reviews addressing the relationship between PKM2 and tumorigenesis remain limited. This review systematically examines the biological functions of PKM2, the signalling mechanisms through which it exerts its effects in malignant tumours, and the latest advances in the development of PKM2-targeted therapeutics, offering insights into potential directions for future drug discovery.
Keywords: M2-type pyruvate kinase, aerobic glycolysis, PKM2-targeted therapeutics, signaling networks, anti-cancer
Received: 18 Jun 2025; Accepted: 26 Sep 2025.
Copyright: © 2025 Liu, Wang, Liang, Chen, Xie and Tang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Wencheng Tang, 46491780@qq.com
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