Efflux pumps, NHE1, monocarboxylate transporters, and ABC transporter subfamily inhibitors

The transporter family of proteins play an essential role in normal physiology of the human body, as well as in many pathological states, generated by genetic or acquired diseases, including many forms of cancer. The chapter details the main classes of transporters, their natural substrates, and the drugs that can be transported in/out of various cells. It also details the classes of inhibitors developed against each type of transporter, their potency, selectivity and toxicity, alone and in combination with different other drugs, in vitro and in vivo. Whenever possible, we have presented the translational efforts made to move different transporter inhibitors into clinical use, as well as the representatives currently available in clinic, their advantages and limitations.