Target intelligence / Profile preview

L-Lactate (Lactate)

Target
Lactate
Molecular classification
Metabolite, Carboxylic acid, Oncometabolite, Signaling molecule
01

Overview

Extracellular lactate is a central component of the metabolic reprogramming observed in malignant tumors, where it accumulates as a byproduct of the Warburg effect (Liberti & Locasale, 2016). Beyond its role as a waste product, it functions as a key oncometabolite that acidifies the tumor microenvironment (TME), facilitating protease activation and basement membrane degradation to promote metastasis (de la Cruz-López et al., 2019). Lactate also mediates metabolic symbiosis between glycolytic and oxidative cancer cells and serves as a ligand for the G protein-coupled receptor GPR81, which triggers pro-survival signaling (Brown et al., 2020). Crucially, high lactate levels create an immunological desert by suppressing the effector functions of T cells and NK cells, thereby enabling immune evasion (Brand et al., 2016). Current drug development efforts focus on small molecule inhibitors of monocarboxylate transporters (MCT1/4) and lactate dehydrogenase (LDHA) to disrupt these metabolic and signaling axes (Halestrap, 2013).

Other names
Lactic acid2-hydroxypropanoateOncometabolite lactateExtracellular lactate
02

Mechanism of action

Inhibition of monocarboxylate transporters (MCT1/4) to block lactate transport or inhibition of lactate dehydrogenase (LDH) to prevent lactate synthesis.

03

Biological functions

Energy metabolismImmune modulationAngiogenesispH regulationCell signaling
04

Disease associations

CancerInflammationSepsisIschemia
05

Safety considerations

Systemic lactic acidosisExercise intoleranceMetabolic toxicityGastrointestinal distress
06

Interacting drugs

AZD3965

4 more in the full profile.

07

Biomarkers

Serum lactate concentrationLactate dehydrogenase (LDH) levelsMCT1 expressionMCT4 expression

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