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Target intelligence / Profile preview
Pyruvate Kinase M2 Isoform (PKM2)
- Target
- PKM2
- Molecular classification
- Enzyme, Kinase
01
Overview
Pyruvate kinase M2 (PKM2) is an isoform of pyruvate kinase that catalyzes the final step of glycolysis, converting phosphoenolpyruvate to pyruvate and generating ATP. It plays critical roles in cellular energy production, anabolic metabolism, and gene expression regulation, particularly in proliferating cells and cancer cells. Its dysregulation is implicated in cancer development, inflammation, and other metabolic diseases, making it a potential therapeutic target.
- Other names
- Pyruvate kinase muscle type 2PKMTumor M2-PK
02
Mechanism of action
Inhibition of enzymatic activity; modulation of tetramer-dimer equilibrium; interference with nuclear translocation or protein interactions.
03
Biological functions
GlycolysisATP productionMetabolic regulationGene expression regulationCell proliferationRedox homeostasisAnabolic precursor supply
04
Disease associations
CancerInflammationMetabolic disorders
05
Safety considerations
Potential for off-target effects due to homology with other pyruvate kinase isoformsDisruption of normal cellular metabolismCompensatory mechanisms in cancer cells leading to resistance
06
Biomarkers
PKM2 expression levels in tumor tissueSerum PKM2 levelsRatio of PKM2 tetramer to dimer
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