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. 2013 Nov 15;33(6):e00080. doi: 10.1042/BSR20130066

Figure 2. Main targets of 3BP in tumour cell.

Figure 2

3BP is incorporated by MCT1 and reacts with this monocarboxylate transporter blocking lactate efflux ([44], see also the metabolomic data of this citation); (2) 3BP acts at distinct steps of ATP-producing enzymes, i.e. GA3PDH, 3PGK, PyK, malate, pyruvate, glutamate and succinate dehydrogenases (MDH, PDH, GDH, SDH, respectively), but does not affect the ATP-using enzymes, i.e. mt-HK, PGI, PFK I and SERCA [48]; (3) small metabolite analogues of the energy metabolism of tumour are not good substrates of efflux pumps involved in the chemotherapeutic resistance of several tumour cell lines. This peculiarity would facilitate the uptake and accumulation in cancer cells. The cellular redox system of reduced/oxidized glutathione levels [GSH]/[GSSG]cyt/mito in cytoplasmic and mitochondrial compartments would play a role in 3BP mechanism of killing tumours cells. In addition to the amount of MCT 1, the amount of mt-HK binding to VDAC/ANT/FoF1ATP synthase would set the mitochondrial state more amenable to 3BP alkylation reaction.