Transportertargeted

Transportertargeted is a term used to describe strategies that focus on membrane transport proteins as primary targets or conduits for therapy, diagnostics, and drug delivery. Transporters regulate the movement of substrates such as nutrients, metabolites, and drugs across cellular membranes, profoundly shaping pharmacokinetics, tissue distribution, and therapeutic efficacy. Major transporter families include the ATP-binding cassette (ABC) transporters, which often mediate efflux and can contribute to drug resistance, and the solute carrier (SLC) transporters, many of which facilitate cellular uptake.

Applications of transportertargeted approaches span several areas. Direct modulation of transporter activity aims to increase drug exposure in target tissues (for example, inhibiting efflux transporters to improve brain or tumor drug delivery). Prodrug and substrate strategies exploit specific transporters to enhance oral absorption or tissue uptake by converting a drug into a transporter-recognized form. Transporter‑targeted delivery systems use ligands or nanoparticle formulations designed to enter cells via particular transporters, potentially improving selectivity and distribution. In imaging, transporter-targeted radioligands or probes enable visualization of transporter expression or function in vivo.

Examples and challenges accompany this field. P-glycoprotein and other efflux transporters are common targets in attempts to overcome multidrug resistance. Nucleoside and other transporter substrates are used to improve pharmacokinetics, while uptake transporters like GLUT and various SLC members influence CNS and organ delivery. Challenges include overlapping substrate specificities, species differences in transporter expression, compensatory mechanisms, and safety concerns related to broad transporter modulation.

See also: membrane transport proteins, pharmacokinetics, drug delivery, transporter inhibitors.