Arsenic-Based Antineoplastic Drugs and Their Mechanisms of Action

Figure 1

Many vicinal thiol-containing redox proteins are major mitochondrial targets for binding of arsenic-containing compounds. Arsenite and particularly organic arsenites will disrupt the normal redox systems functioning in the mitochondrial matrix and intermembrane space by targeting vicinal thiols in proteins and enzymes that regulate these systems. Such enzymes include Peroxiredoxin III (Prx III), Thioredoxin 2 (Trx2). In addition, several key mitochondrial functions are affected, including Factor B regulating the ATP synthetase activity, the adenine nucleotide transporter, ANT, amongst others. See text for further detail.