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Multidrug efflux systems export a wide a variety of substrates from cells and consequently are capable of conferring resistance to a wide range of chemotherapeutic agents. Multidrug resistance caused by active drug efflux is one of the major clinical impediments in anti-cancer chemotherapy and treatment of infectious diseases. Multidrug exporters are ubiquitously expressed in prokaryotic and eukaryotic organisms where they regulate absorption, distribution and excretion of xenobiotics, and protect sanctuary tissues by regulating the drug permeability of the blood-brain, -placenta and -testis barriers. In addition to regulating pharmacokinetics, transporters are also major players in dictating tissue-responses to drugs, from pharmacological efficacy to toxicity.

Targeting the Mechanisms and Regulation of Transporters for Advancing Health During a Pandemic