Drug transport protein (DTP)

Drug transport proteins are specialized membrane proteins that regulate the movement of drugs and endogenous molecules across biological membranes (StatPearls, 2023). They are primarily divided into two major superfamilies: the ATP-binding cassette (ABC) transporters, which function as primary active efflux pumps, and the Solute Carrier (SLC) transporters, which facilitate the uptake or exchange of solutes (UniProt, 2024). These proteins are critical determinants of a drug's pharmacokinetics, influencing absorption in the gastrointestinal tract, distribution across the blood-brain barrier, and elimination via the liver and kidneys (NIH, 2022). In clinical oncology, the overexpression of efflux transporters such as P-glycoprotein is a well-documented mechanism of multidrug resistance in cancer cells (PubMed, 2021). Furthermore, these transporters are the site of significant drug-drug interactions, where the inhibition or induction of a transporter by one drug can lead to toxic levels or sub-therapeutic concentrations of another (FDA, 2020). Therapeutic targeting of these proteins has led to the development of important drugs, such as SGLT2 inhibitors for managing type 2 diabetes and URAT1 inhibitors for treating gout (Nature Reviews Drug Discovery, 2020). Genetic polymorphisms in transporter genes can also lead to significant inter-individual variability in drug response and susceptibility to adverse effects.

Other names

Membrane transporterXenobiotic transporterEfflux pumpUptake transporterABC transporterSLC transporter

Drug transport proteins modulate the movement of substrates across cellular membranes through various mechanisms, including primary active transport driven by ATP hydrolysis, secondary active transport utilizing ion gradients, and facilitated diffusion (StatPearls, 2023).