Figure 5.

Therapeutic approaches involving isoforms monocarboxylate transporter (MCT)1 and MCT4. (a) MCT1 expression can be exploited for targeted drug delivery (e.g., of 3‐bromopyruvate), into MCT1 expressing tumor cells. (b) MCT4 represents an attractive target for inhibition in tumor cells. Compounds, such as bindarit or modified derivatives, represent promising candidates. (c) Targeted DNA methylation of the hypomethylated SLC16A3 promoter, mediated, for example, by a CRISPR‐dCas9‐DNMT construct, might represent an alternative approach to restore normal MCT4 expression levels in tumor cells.