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In human colon cancer cells, glycolytic activity shows a positive correlation with proliferation. Regulation of glycolysis is exerted particularly at the level of phosphofructokinase 1. That enzyme is activated by fructose 2,6-bisphosphate the levels of which are controlled by the bifunctional enzymes with phosphofructosekinase 2 and fructose 2,6-biphosphatase activities (PFKFBs). PFKFB3 is an important enzyme regulating glycolysis in many tumor cells. We have studied the action of 3-(3-pyridinyl)-1-(4pyridinyl)-2-propen-1-one (3PO), an inhibitor of PFKFB3, as a single agent and in combination with other molecules that affect glycolysis and proliferation in four colon cancer cell lines (Caco-2, HCT116, HT29 and SW1116). The molecules studied were 3-bromopyruvate, butyrate, 2-deoxyglucose, and the biguanides metformin and phenformin that have been found previously to inhibit the proliferation of colon cancer cells [1-3].

journal of cancer research and therapy

Inhibition of glycolysis and growth of colon cancer cells by 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one (3PO) in combination with butyrate, 2-deoxy glucose, 3-bromopyruvate or biguanides