Overview of Drug Transporter Families

Microarray Determination of the Expression of Drug Transporters in Humans and Animal Species Used for the Investigation of Nasal Absorption

“…The activity of transporters, however, is not limited only to their physiological substrates but also includes a variety of exogenous compounds. Drugs with structural similarities to endogenous transporter substrates can also be transported across cell membranes thus modulating their absorption, disposition, and elimination …”

“…The transporters of greatest current interest in drug disposition belong to one of two major classes: ATP-binding cassette (ABC) and solute carrier (SLC) transport families. ABC transporters are primarily active transporters that mediate the efflux of compounds out of cells, , and the overexpression of ABC transporters has long been known to be related to drug resistance. − The most studied drug transporters belonging to the ABC family include multidrug resistance protein 1 (MDR1) or P-glycoprotein (P-gp), the multidrug resistance-associated proteins 1–9 (MRPs 1–9), and breast cancer resistance protein (BCRP). The majority of known drug uptake transporters belong to the SLC transporter family.…”

“…The majority of known drug uptake transporters belong to the SLC transporter family. Among the families that have been studied extensively for their role in drug absorption, the organic cation, organic cation/carnitine, organic anion, peptide, monocarboxylate, and nucleoside transporters are of particular current interest . The amino acid transporters, another SLC family, are divided into two subfamilies: the cationic amino acid transporters (CAT family, SLC7A1–4) and the glycoprotein-associated amino acid transporters (gpaAT family, SLC7A5–7), which are heterodimeric amino acid transporters (HAT) .…”

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates

“…160,161 Recent advances in molecular biology have enabled the identification of more than 400 membrane transporters in the human genome, which has contributed to an increased understanding of their expression in specific tissues, their regulation, their mechanisms of transport, their substrates and inhibitors, and species-dependent differences in activity and function. 162 Transporters are involved in the uptake and efflux of endogenous substances including physiological chemicals, nutrients, and ions, but can also transport xenobiotics. Transporters expressed on both the apical and basolateral sides of intestinal enterocytes that can influence the oral absorption of drugs include oligopeptide transporter (PepT), organic anion transporter (OAT), organic cation transporter (OCT), sodium-dependent glucose transporter (SGLT) family, apical sodium-dependent bile acid transporter, monocarboxylate transporter, proton-coupled amino acid transporter, and amino acid transporter ATB° ,+ .…”

“…Transporters expressed on both the apical and basolateral sides of intestinal enterocytes that can influence the oral absorption of drugs include oligopeptide transporter (PepT), organic anion transporter (OAT), organic cation transporter (OCT), sodium-dependent glucose transporter (SGLT) family, apical sodium-dependent bile acid transporter, monocarboxylate transporter, proton-coupled amino acid transporter, and amino acid transporter ATB° ,+ . 160–162 Peptide transporters, especially PepT1, have drawn significant attention in drug discovery since targeting this transporter remains an attractive strategy for improving oral drug delivery based on its abundant expression in the small intestine, high substrate capacity, and broad substrate specificity. These properties are reflected in the PepT1-mediated transport of a wide range of substrates that include dipeptides, tripeptides, β-lactam antibiotics, angiotensin-converting enzyme inhibitors, and antiviral drugs.…”