Halestrap · IUBMB life 2012 · narrative review · n=?

The monocarboxylate transporter family--Structure and functional characterization.

Cited 708 times in the scientific literature.

Level 5 - mechanism / opinion, no new human data

Narrative review of biochemical and structural mechanistic studies.

PubMed 22131303 · doi:10.1002/iub.573 · record verified 2026-08-30

What was done

This narrative review summarizes structural and biochemical findings on the 14-member monocarboxylate transporter (MCT / SLC16) family. It details the structural topology, catalytic mechanisms, and chaperone protein requirements of monocarboxylate-transporting isoforms (MCT1–4) derived from labeling studies, proteolytic digestion, site-directed mutagenesis, and molecular modeling.

What was found

The abstract reports qualitative mechanistic properties rather than numerical data. MCTs 1–4 facilitate proton-linked transport of L-lactate, pyruvate, and ketone bodies. Structural mapping confirms a 12-transmembrane helix topology with intracellular termini and a large intracellular loop between helices 6 and 7. Proper plasma membrane translocation and catalytic activity of MCT1–4 require association with single-transmembrane immunoglobulin chaperones: MCT1, MCT3, and MCT4 bind preferentially to basigin, whereas MCT2 binds to embigin. Chaperone association alters inhibitor specificity but does not modify substrate kinetics.

Why it matters

Understanding the structural conformations and required chaperone interactions of MCTs provides a mechanistic baseline for targeting cellular metabolic transport (such as lactate shuttling) in disease states.

Limits

The abstract provides no quantitative metrics or statistical evaluations. Findings reflect in vitro biochemical and structural models rather than clinical trial data, and eight of the 14 SLC16 family members remained uncharacterized orphan transporters at the time of review.

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