FIGURE 4.

Interaction of monocarboxylates with SLC5A8 and GPR109A. A, selectivity of monocarboxylates as inhibitors of HDAC. SW480 cell lysates were used as the source of HDAC activity. The dose-dependent effects of acetate, propionate, butyrate, and nicotinate on HDAC activity were monitored in a cell-free system using a commercially available kit (BioVision). B, selectivity of monocarboxylates as agonists for human GPR109A. The agonist selectivity of acetate, propionate, butyrate, and nicotinate on GPR109A was monitored using the BRET assay. The concentration of monocarboxylates in the assay was 5 mm. C, differential features of monocarboxylates in terms of selectivity as substrates of human SLC5A8 and agonists for human GPR109A and ability to inhibit HDACs.