癌细胞采用糖酵解表型来满足不利条件下的能量需求。在代谢重连中，癌细胞将糖酵解途径调节因子的表达上调，包括葡萄糖转运蛋白 1、己糖激酶 2 和 PKM2（丙酮酸激酶），使其形成 M2 剪接形式。在这些调节因子中，PKM2 在代谢重编程中发挥着重要作用，并且在包括癌症在内的各种疾病中过度表达。 PKM2 的二聚化导致糖酵解中间体生成合成前体，这对于细胞生长和癌细胞增殖至关重要。本文重点研究 PKM2 激活剂、抑制剂及其生物和合成特性的最新专利（2018-2023），方法是使用欧洲专利局 (EPO) 的高级检索服务。此外，还检查了 PubMed、Google Scholar 和 Elsevier 等其他数据库的科学数据。根据其化学结构，PKM2激活剂和抑制剂分为吡唑、吡咯烷-吡唑、苯酚、苯并恶嗪、异硒唑并吡啶鎓、酞嗪和丙酰胺衍生物。激活PKM2通过减少细胞增殖和发育所需的生物分子数量来减少细胞增殖和发育。细胞形成。 PKM2 激活剂和抑制剂对于治疗许多癌症病原体非常有效。寻找新的、更有效的和选择性的分子来激活和抑制 PKM2 非常重要。

Cancer cells adopt a glycolytic phenotype to fulfill their energy needs in unfavorable conditions. In metabolic rewiring, cancer cells upregulate the expression of glycolytic pathway regulators including glucose transporter 1, hexokinase 2, and PKM2 (pyruvate kinase) into its M2 splice form. Among these regulators, PKM2 plays a major role in metabolic reprogramming and is overexpressed in various diseases, including cancer. Dimerization of PKM2 causes the generation of synthetic precursors from glycolytic intermediates, which are essential for cellular growth and cancer cell proliferation.This article is focused on examining recent patents (2018-2023) on PKM2 activators, inhibitors and their biological and synthesis properties by using the advanced search service of the European Patent Office (EPO). Moreover, other databases including PubMed, Google Scholar and Elsevier were also examined for scientific data. On basis of their chemical structures, PKM2 activators and inhibitors are classified into pyrazole, pyrolidine-pyrazole, phenol, benzoxazine, isoselenazolo-pyridinium, phthalazine, and propiolylamide derivatives.Activating PKM2 reduces proliferation and development of cells by reducing the quantity of biomolecules needed for cell formation. PKM2 activators and inhibitors are highly effective in treating many cancer pathogens. It is important to find new, more potent and selective molecules for PKM2 activation and inhibition.