The article "Mammalian ABC transporters in health and disease" by Borst and Oude Elferink provides an in-depth review of the roles of ATP-binding cassette (ABC) transporters in human physiology, toxicology, pharmacology, and disease. ABC transporters are large membrane proteins that use energy from ATP hydrolysis to transport a variety of compounds across cell membranes, including lipids, bile salts, toxic compounds, and peptides. The human genome contains 48 ABC genes, with 16 having known functions and 14 associated with human diseases. These transporters are essential for maintaining physiological balance and are involved in drug resistance, lipid transport, and the excretion of harmful substances. The review highlights the importance of ABC transporters in drug transport, particularly in the context of multidrug resistance (MDR) in cancer cells. P-glycoprotein (Pgp), MRP1, and BCRP (ABCG2) are key transporters involved in this process. Pgp is known for its ability to transport a wide range of drugs, including many chemotherapeutic agents, out of cells, thereby reducing their intracellular concentration and contributing to drug resistance. BCRP, another ABC transporter, is also involved in drug resistance and has a broader range of substrates compared to Pgp. The article also discusses the role of ABC transporters in the excretion of substances by secretory epithelia, such as the liver, where they help in the transport of bile salts, phosphatidylcholine, and drugs. Defects in ABC transporter genes are associated with various inborn diseases, including cystic fibrosis and certain forms of liver disease. Additionally, ABC transporters are under tight transcriptional regulation by nuclear receptors, which is particularly important for lipid transporters and MDR1 and MRP2. The review emphasizes the biochemical mechanisms and genetic defects underlying ABC transporter function, as well as their significance in human health and disease. It also discusses the challenges in understanding the precise mechanisms of ABC transporter function, including the structure and dynamics of these proteins. The article concludes with the importance of ABC transporters in drug transport, their role in disease, and the need for further research to fully understand their functions and potential therapeutic applications.The article "Mammalian ABC transporters in health and disease" by Borst and Oude Elferink provides an in-depth review of the roles of ATP-binding cassette (ABC) transporters in human physiology, toxicology, pharmacology, and disease. ABC transporters are large membrane proteins that use energy from ATP hydrolysis to transport a variety of compounds across cell membranes, including lipids, bile salts, toxic compounds, and peptides. The human genome contains 48 ABC genes, with 16 having known functions and 14 associated with human diseases. These transporters are essential for maintaining physiological balance and are involved in drug resistance, lipid transport, and the excretion of harmful substances. The review highlights the importance of ABC transporters in drug transport, particularly in the context of multidrug resistance (MDR) in cancer cells. P-glycoprotein (Pgp), MRP1, and BCRP (ABCG2) are key transporters involved in this process. Pgp is known for its ability to transport a wide range of drugs, including many chemotherapeutic agents, out of cells, thereby reducing their intracellular concentration and contributing to drug resistance. BCRP, another ABC transporter, is also involved in drug resistance and has a broader range of substrates compared to Pgp. The article also discusses the role of ABC transporters in the excretion of substances by secretory epithelia, such as the liver, where they help in the transport of bile salts, phosphatidylcholine, and drugs. Defects in ABC transporter genes are associated with various inborn diseases, including cystic fibrosis and certain forms of liver disease. Additionally, ABC transporters are under tight transcriptional regulation by nuclear receptors, which is particularly important for lipid transporters and MDR1 and MRP2. The review emphasizes the biochemical mechanisms and genetic defects underlying ABC transporter function, as well as their significance in human health and disease. It also discusses the challenges in understanding the precise mechanisms of ABC transporter function, including the structure and dynamics of these proteins. The article concludes with the importance of ABC transporters in drug transport, their role in disease, and the need for further research to fully understand their functions and potential therapeutic applications.