Mammalian transporter

Mammalian transporters are a vast class of membrane proteins that facilitate the movement of ions, nutrients, and xenobiotics across biological membranes (UniProt, 2024). They are broadly divided into the Solute Carrier (SLC) superfamily, which includes over 400 members, and the ATP-Binding Cassette (ABC) superfamily (Hediger et al., 2013). These proteins are essential for maintaining cellular homeostasis, regulating pH, and managing the uptake of vital substances like glucose and amino acids (NIH, 2023). In the context of pharmacology, transporters are critical components of the ADME (Absorption, Distribution, Metabolism, and Excretion) profile of drugs, often determining the bioavailability and tissue distribution of therapeutic agents (Giacomini et al., 2010). Many transporters are direct therapeutic targets, such as the serotonin transporter (SERT) for antidepressants or the sodium-glucose cotransporter 2 (SGLT2) for diabetes (PubMed, 2023). However, they are also frequent sites of drug-drug interactions, where one drug inhibits the transport of another, leading to potential toxicity (FDA, 2020). Genetic polymorphisms in transporter genes can significantly impact individual drug responses and disease susceptibility (StatPearls, 2024).

Other names

Membrane transporterSolute carrier (SLC)ATP-binding cassette transporter (ABC transporter)Ion transporterDrug transporter

Inhibition of substrate translocation, competitive inhibition at the binding site, non-competitive or allosteric modulation of transport activity, and induction or repression of transporter expression (Giacomini et al., 2010; PubMed, 2023).