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Synthesize current evidence on the regulation, structure, and biological functions of monocarboxylate transporters (MCTs) in tumor lactate metabolism, signaling, and cancer progression.

July 27, 2019Molecular MetabolismOpen Access

Monocarboxylate transporters in cancer

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Synthesize current evidence on the regulation, structure, and biological functions of monocarboxylate transporters (MCTs) in tumor lactate metabolism, signaling, and cancer progression.
Narrative review synthesizing mechanisms of tumor metabolic plasticity, monocarboxylate transporter isoforms (MCT1–4), and lactate signaling via the cell surface receptor GPR81.
Evaluation of preclinical animal models and human genetic data to assess the therapeutic feasibility of pharmacological MCT inhibition.
Lactate functions as both an oxidative metabolic fuel and a signaling molecule that promotes tumor angiogenesis and metastasis via MCT-gated transport and GPR81 receptor activation.
Targeting lactate transport is clinically druggable, with selective MCT1 inhibitors in advanced clinical development and MCT4 inhibitors in discovery phases.
Non-invasive monitoring of tumor lactate fluxes using positron emission tomography tracers offers a strategy to identify patients most likely to respond to MCT-targeted therapies.

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Review uncovers monocarboxylate transporter roles in cancer metabolism and signaling, highlighting their therapeutic potential as druggable targets.

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Payen et al. (2019) studied this question.

synapsesocial.com/papers/6a09f3be87ad1657d251e2d4 https://doi.org/10.1016/j.molmet.2019.07.006

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Implication

Review uncovers monocarboxylate transporter roles in cancer metabolism and signaling, highlighting their therapeutic potential as druggable targets.

Monocarboxylate transporters in cancer

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Monocarboxylate transporters in cancer

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