Here, we focus on three cancer-specific therapeutic target molecules: two kinases, namely, maternal embryonic leucine zipper kinase (MELK) and T-lymphokine-activated killer cell-originated protein kinase (TOPK); and one scaffold anchoring protein, namely, brefeldin A-inhibited guanine nucleotide-exchange protein 3 (BIG3). The gene discussed is ARFGEF3; the disease is cancer.