Human drug transporters

Human drug transporters are a vast group of membrane proteins that regulate the entry and exit of drugs and endogenous molecules across cellular membranes. They are broadly classified into two superfamilies: the Solute Carrier (SLC) family, which primarily mediates the uptake of molecules into cells, and the ATP-Binding Cassette (ABC) family, which utilizes ATP hydrolysis to pump substrates out of cells against concentration gradients [1][2]. These transporters are highly expressed in pharmacologically relevant tissues, including the intestinal epithelium, hepatocytes, renal proximal tubules, and the endothelial cells of the blood-brain barrier [3]. By controlling the movement of xenobiotics, they play a decisive role in the pharmacokinetics of a wide range of medications, influencing their absorption, distribution, and elimination [4]. Clinically, they are major determinants of drug-drug interactions (DDIs), as many drugs act as substrates or inhibitors of these proteins, potentially leading to toxic accumulations or sub-therapeutic levels [5]. Furthermore, certain transporters like P-glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2) are well-known for their role in multidrug resistance in oncology [6].

Other names

Membrane transportersXenobiotic transportersABC transportersSLC transportersEfflux and uptake transporters

Substrate for transport, competitive inhibition, non-competitive inhibition, and transcriptional induction [3][5].