Cancer cells are characterized by reprogramming of energy metabolism. Over the last decade, understanding of the metabolic
changes that occur in cancer has increased dramatically, with great interest in targeting metabolism for cancer therapy. Pyruvate kinase
isoenzyme type M2 (abbreviations: PKM2, M2-PK) plays a key role in modulating glucose metabolism to support cell proliferation.
PKM2, like other PK isoforms, catalyzes the last energy-generating step in glycolysis, but is unique in its capacity to be regulated. PKM2
is regulated at several cellular levels, including gene expression, alternative splicing and post-translational modification. In addition,
PKM2 is regulated by key metabolic intermediates and interacts with more than twenty different proteins. Hence, this isoenzyme is an
important regulator of glycolysis, and additionally functions in other novel roles that have recently emerged. Recent evidence indicates
that intervening with the complex regulatory network of PKM2 has severe consequences on tumor cell proliferation, indicating the potential
of this enzyme as a target for tumor therapy.