Abstract: Tumor cells always undergo glycolysis to metabolize glucose even in the presence of oxygen, which is termed aerobic glycolysis, also known as Warburg effect. A key sensor regulator of this process is pyruvate kinase M2 (PKM2), which catalyzed the PEP to pyruvate. It is particularly expressed in proliferative cells especially in tumor cells. It is always switched between a highly active tetrameric form and a nearly low active dimeric form, which determined whether the glucose carbons are converted to pyruvate under the production of energy or participated into synthetic processes. In tumor cells, the dimeric form of PKM2 is predominant. The amounts of Tumor M2-PK can serve as a biomarker to be detected in EDTA-plasma and stool samples of patients with various types of cancers. PKM2 is a pTyr-binding protein; it can be regulated by a lot of transcription factors such as HIF1α, and metabolic intermediates such as FBP. The crucial role of PKM2 in tumor glucose metabolism and proliferation makes it an interesting therapeutic target for the treatment of human cancers.

Key words: aerobic glycolysis (Warburg effect), PKM2, tumor development