Target intelligence / Profile preview

Monocarboxylate transporter 2 (MCT2) (MCT2)

Target
MCT2
Molecular classification
Transporter, Solute carrier family
01

Overview

Monocarboxylate transporter 2 (MCT2), encoded by the SLC16A7 gene, is a high-affinity transmembrane protein responsible for the transport of monocarboxylates such as lactate, pyruvate, and ketone bodies across the plasma membrane [UniProt: O60669]. It plays a vital role in cellular metabolism, particularly in the brain where it facilitates the uptake of lactate by neurons to support oxidative phosphorylation, a process known as the astrocyte-neuron lactate shuttle [PubMed: 22130306]. In many cancers, including glioblastoma and prostate cancer, SLC16A7 is significantly upregulated to meet the high metabolic demands of tumor cells and to manage the acidic byproducts of aerobic glycolysis [PubMed: 25825575]. Targeting the SLC16A7 mRNA or the resulting MCT2 protein offers a therapeutic strategy to disrupt tumor metabolism and induce cell death by inhibiting the efflux of lactate or the influx of metabolic fuels. While potent small-molecule inhibitors like AR-C155858 have demonstrated efficacy in preclinical models, the high expression of MCT2 in the central nervous system poses significant challenges for clinical safety and drug delivery [PubMed: 20443793]. Current research also explores the use of RNA interference (siRNA) to specifically knockdown SLC16A7 mRNA as a means of precision metabolic therapy in oncology.

Other names
SLC16A7Monocarboxylate transporter 2Solute carrier family 16 member 7MCT 2SLC16A7 mRNA
02

Mechanism of action

Inhibition of monocarboxylate transport across the plasma membrane, disrupting cellular pH regulation and metabolic fuel supply; mRNA-targeted therapies like siRNA or antisense oligonucleotides aim to reduce protein expression levels [PubMed: 20443793].

03

Biological functions

Lactate transportPyruvate transportKetone body transportMetabolic reprogrammingTransmembrane transportpH regulation
04

Disease associations

CancerGlioblastomaProstate cancerEpilepsyNeurodegenerative disease
05

Safety considerations

Potential neurotoxicity due to high expression in neuronsMetabolic acidosisOff-target inhibition of other MCT isoforms (MCT1, MCT4)Disruption of the astrocyte-neuron lactate shuttle
06

Interacting drugs

AR-C155858

3 more in the full profile.

07

Biomarkers

MCT2 protein expression (IHC)SLC16A7 mRNA levelsIntracellular lactate concentrationFDG-PET imaging (indirectly via metabolic shift)

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