ATP-binding cassette transporter (ABC transporter) (ABC transporter)

ATP-binding cassette (ABC) transporters are a large superfamily of membrane proteins that utilize the energy of ATP hydrolysis to transport a wide variety of substrates across cellular membranes (NIH, 2022). In humans, there are 48-49 identified ABC transporters categorized into seven subfamilies (ABCA-ABCG), playing essential roles in nutrient uptake, lipid homeostasis, and the detoxification of xenobiotics (UniProt, 2023; StatPearls, 2023). These proteins are critical in pharmacology as they influence the absorption, distribution, and elimination of many drugs, and their overexpression is a primary cause of multidrug resistance (MDR) in cancer (PubMed, 2021). Mutations in ABC transporter genes are linked to numerous genetic disorders, including cystic fibrosis (CFTR/ABCC7), Stargardt disease (ABCA4), and Tangier disease (ABCA1) (NIH, 2002). Therapeutic strategies include the use of modulators to restore function in genetic defects or inhibitors to sensitize cancer cells to chemotherapy (Nature Reviews Drug Discovery, 2020). Additionally, they serve as important barriers in the blood-brain barrier and placenta, protecting sensitive tissues from toxic insults (ResearchGate, 2023).

Other names

ABC proteinTraffic ATPaseATP-binding cassette superfamilyABC transporters

ATP-dependent primary active transport of substrates across biological membranes against concentration gradients; some members function as ion channels or regulators of other channels (e.g., CFTR, SUR1) (NIH, 2022; StatPearls, 2023).