Unlike normal cells, cancer cells have been noted to shift their energy metabolism toward glycolysis. This phenomenon, originally termed the Warburg effect, allows cancer cells to satisfy increased biosynthetic requirements for biomass and energy. The HIF-1-induced PFKFB3 (EC 2.7.1.105) plays a key role in this adaptation of cancer cells to adopt glycolysis as the major source of metabolic energy production for fast cell growth. It does so by elevating the concentration of Fru-2,6-BP, the most potent glycolysis stimulator. As this metabolic conversion has been suggested to be a hallmark of cancer, PFKFB3 has emerged as a novel target for cancer chemotherapy[1].