Tumor cells were exposed to different agents capable of targeting pH regulators, monocarboxylate transporters, enzymes catalyzing glycolysis and Krebs’ cycle, cyclooxygenases, and fatty acid synthase both in vitro and in vivo, followed by analysis of cell survival parameters, and underlying molecular mechanisms of tumor growth retardation and chemosensitization. The gene discussed is FASN; the disease is neoplasm.