Due to its high expression in many solid tumors and its role in the reductive activation of anti-cancer agents such as mitomycin C (6-amino-1,1a,2,8,8a,8b-hexahydro-8-(hydroxymethyl)-8a-methoxy-5-methyl-azirino[2′,3′:3,4]pyrrolo[1,2-a]indole-4,7-dione carbamate), E09 (3-hydroxy-5-aziridinyl-1-methyl-2-(1H-indole-4,7-dione)-prop-β-en-α-ol) and β-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione), NQO1 constitutes an attractive target for selective anti-cancer drug development. The gene discussed is NQO1; the disease is cancer.