Medicinal Chemistry - Fusion of Traditional and Western Medicine

Volume: 2

Second Edition

Indexed in: Book Citation Index, Science Edition, EBSCO.

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Drugs That Target Transporters, Carriers and Ion Pumps

Pp. 416-424 (9)

Robert E. Smith


Another important class of proteins that make good targets for drugs is the class that contains transporters, carriers and ion pumps. There are several drugs that affect ion pumps, carriers and transporters. Ezetimibe (Zetia®) inhibits the absorption of dietary cholesterol in the small intestines. Stomach acid is produced by one type of H+/K+ ATPase. The drugs called Omeprazole (Prilosec®) and Prevacid inactivate it. Atovaquone and Proguanil act by inhibiting electron transport. Ion pumps are also important in multidrug resistant (MDR) bacteria and cancer cells. Ivermectin (Stromectol®) is a broad spectrum antiparasitic agent that acts by opening glutamategated chloride channels in invertebrates. MDR in cancer involves simultaneous resistance to several different, unrelated anticancer drugs. An efflux protein, P glycoprotein, or PgP, pumps out anticancer drugs. There are several other drugs, called MDR converters that inhibit the action of PgP.


Ezetimibe, H+/K+ ATPase, Omeprazole, Prevacid, Ivermectin, multidrug resistance.


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