Target intelligence / Profile preview

Pyruvate kinase muscle isoform 2 (PKM2)

Target
PKM2
Molecular classification
Enzyme, Kinase, Metabolic enzyme, Transcription factor coactivator
01

Overview

Pyruvate kinase muscle isoform 2 (PKM2) is a key glycolytic enzyme catalyzing the final step of glycolysis. It is predominantly expressed in embryonic tissues, adult proliferating cells, tumor cells, and certain normal proliferating cell types. PKM2 exists in monomeric, dimeric, or tetrameric forms, with the tetrameric form being highly active. It plays crucial roles in cancer metabolism, inflammation, and immune regulation, making it an important therapeutic target.

Other names
Pyruvate kinase isozyme M2Tumor M2-PKPKMPK3
02

Mechanism of action

Inhibition of PKM2 activity, modulation of PKM2 oligomerization

03

Biological functions

GlycolysisATP productionCell proliferationAnabolic metabolismImmune regulationAngiogenesisInflammation regulation
04

Disease associations

CancerInflammationAutoimmune diseasesMetabolic disorders
05

Safety considerations

Potential for off-target effects due to PKM2's role in normal cell metabolismDevelopment of resistance to PKM2 inhibitorsCompensatory mechanisms that bypass PKM2 inhibition
06

Biomarkers

PKM2 expression levels in tumorsPKM2 serum levels

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