丙酮酸激酶 M2 (PKM2) 是丙酮酸激酶 (PK) 的一种亚型，已被证明在癌症的发展中发挥重要作用。它调节糖酵解途径的最后一步。 PKM2同时具有丙酮酸激酶和蛋白激酶活性，PKM2这两种功能的转换依赖于二聚体和四聚体的相互变化。 PKM2的二聚化可以促进肿瘤细胞的增殖和生长，因此抑制PKM2的二聚化对于治疗癌症至关重要。 PKM2 的聚集受到内源和外源辅因子以及翻译后修饰 (PTM) 的调节。尽管关于PKM2在肿瘤发生过程中不同聚集的研究较多，但近年来的总结较少。在这篇综述中，我们首先介绍PKM2在肿瘤生长的各种生物学过程中的作用。然后，我们总结了各种内源性辅因子如果糖-1,6-二磷酸（FBP）、各种氨基酸和翻译后修饰（PTM）对PKM2的聚集调节机制。最后总结了PKM2的相关抑制剂和激动剂，为今后在癌症治疗中调控PKM2聚集提供参考。© 2024。作者获得纳瓦拉大学独家许可。

Pyruvate kinase M2 (PKM2), a subtype of pyruvate kinase (PK), has been shown to play an important role in the development of cancer. It regulates the last step of glycolytic pathway. PKM2 has both pyruvate kinase and protein kinase activity, and the conversion of these two functions of PKM2 depends on the mutual change of dimer and tetramer. The dimerization of PKM2 can promote the proliferation and growth of tumor cells, so inhibiting the dimerization of PKM2 is essential to curing cancer. The aggregation of PKM2 is regulated by both endogenous and exogenous cofactors as well as post-translational modification (PTM). Although there are many studies on the different aggregation of PKM2 in the process of tumor development, there are few summaries in recent years. In this review, we first introduce the role of PKM2 in various biological processes of tumor growth. Then, we summarize the aggregation regulation mechanism of PKM2 by various endogenous cofactors such as Fructose-1, 6-diphosphate (FBP), various amino acids, and post-translational modification (PTMs). Finally, the related inhibitors and agonists of PKM2 are summarized to provide reference for regulating PKM2 aggregation in the treatment of cancer in the future.© 2024. The Author(s) under exclusive licence to University of Navarra.