ATP-binding cassette (ABC) transporter Inhibitors

ATP-binding cassette (ABC) transporters are a large and diverse group of transmembrane proteins that use the energy ATP hydrolysis to transport a wide variety of substrates across cellular membranes. These substrates include lipids, bile salts, amino acids, carbohydrates, vitamins, hormones, drugs, and metabolites. ABC transporters are crucial for many physiological processes, such as lipid transport in the liver, drug excretion in the kidneys, and antigen presentation in the immune system. Their role in effluxing xenobiotics and drugs out of cells also makes them key players in multidrug resistance, particularly in cancer cells. The activity of ABC transporters is tightly regulated by cellular signaling pathways, ensuring that substrate transport is coordinated with the cell's metabolic needs and environmental conditions.

Targeting ATP-binding cassette (ABC) transporters for disruption or inhibition has become an important strategy in various research and application fields. In medical research, inhibiting specific ABC transporters, especially those involved in drug resistance, is a strategy to enhance the efficacy of agents in cancer therapy. Pharmacological inhibitors of ABC transporters can be used to increase the bioavailability of drugs by their efflux from target cells. Researchers also target ABC transporters to study their role in physiological processes and disease states, employing a range of inhibitors that can specifically or broadly target these transporters. However, the challenge in targeting ABC transporters lies in their broad substrate specificity and the potential for unintended effects on normal physiological functions, necessitating the development of highly selective and efficient inhibitors.