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Target intelligence / Profile preview
Pyruvate Kinase Isoform M2 (PKM2)
- Target
- PKM2
- Molecular classification
- Enzyme, Kinase
01
Overview
Pyruvate kinase isoform M2 (PKM2) is a key glycolytic enzyme that catalyzes the final step of glycolysis, converting phosphoenolpyruvate to pyruvate and ATP. It is highly expressed in tumor cells and plays a central role in metabolic reprogramming (Warburg effect), promoting aerobic glycolysis to support rapid cell proliferation. PKM2 also has non-metabolic roles, including protein kinase activity and regulation of gene expression. It is considered a promising target for anti-cancer therapies, with strategies focusing on modulating its oligomerization state or inhibiting its kinase activity.
- Other names
- Pyruvate kinase muscle isozyme M2Tumor M2-PK
02
Mechanism of action
Modulation of PKM2 oligomerization; Inhibition of PKM2 kinase activity; Targeting PKM2 nuclear function
03
Biological functions
GlycolysisATP productionProtein phosphorylationRegulation of gene expressionCell proliferationMetabolic reprogrammingImmune response
04
Disease associations
CancerInflammation
05
Safety considerations
Potential for off-target effects due to structural similarity with other pyruvate kinase isoformsDevelopment of resistance to PKM2 inhibitorsToxicity related to disruption of normal cellular metabolism
06
Biomarkers
PKM2 expression levels as a prognostic marker in cancerTumor M2-PK levels in serum as a diagnostic marker
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