Target intelligence / Profile preview

Pyruvate kinase muscle isozyme 2 messenger RNA (PKM2 mRNA)

Target
PKM2 mRNA
Molecular classification
Messenger RNA, Nucleic acid
01

Overview

Pyruvate kinase muscle isozyme 2 (PKM2) mRNA is the transcript of the PKM gene that specifically includes exon 10, a result of alternative splicing that distinguishes it from the PKM1 isoform. This molecule serves as a critical therapeutic target because it encodes the PKM2 protein, a rate-limiting enzyme in glycolysis that is frequently overexpressed in cancer cells to facilitate the Warburg effect. By promoting aerobic glycolysis, PKM2 provides the necessary biosynthetic intermediates and energy for rapid tumor growth and survival. Therapeutic strategies targeting PKM2 mRNA, such as siRNA and antisense oligonucleotides, aim to specifically reduce PKM2 protein levels or shift splicing toward the PKM1 isoform, thereby inhibiting tumor progression and inducing apoptosis. Additionally, PKM2 mRNA plays significant roles in neuroinflammation and cardiac repair, extending its potential utility as a target in regenerative and inflammatory medicine.

Other names
PKM2 transcriptPKM2 pre-mRNAPyruvate kinase M2 mRNAPKM isoform M2 mRNAPyruvate kinase muscle isozyme 2 transcript
02

Mechanism of action

Targeting PKM2 mRNA typically involves RNA interference (RNAi) or antisense-mediated degradation to reduce protein expression, or the use of splice-switching oligonucleotides to favor the production of the PKM1 isoform over PKM2.

03

Biological functions

Glycolysis regulationCell proliferationApoptosis regulationMetabolic reprogrammingInflammatory responseCardiac regenerationOxidative stress modulation
04

Disease associations

CancerNeuroinflammationCardiovascular diseaseAutoimmune diseaseDiabetes
05

Safety considerations

Off-target RNA interactionsSystemic delivery challengesPotential disruption of basal glycolysis in healthy tissuesMetabolic compensation by other glycolytic enzymes
06

Interacting drugs

siRNA (e.g., si156, si27, si155)

6 more in the full profile.

07

Biomarkers

PKM2 protein expression levelsPKM2/PKM1 mRNA ratioLactate concentrationGlucose consumption rateCirculating miR-122 levels

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