Drug transporters in the kidney, liver, intestine, and other organs are among the most studied proteins in the pharmaceutical field due to their role in the absorption, distribution, metabolism and excretion of numerous small molecule drugs. Despite the different physicochemical properties and mechanisms of actions of these drugs, they ultimately depend on a relatively small subset of transporters for their clearance (e.g., OAT1, OATP1B1, P-gp). However, this broad specificity is not limited to pharmaceutical products. It also appears that many of these transporters interact with other types of small molecules (e.g., endogenous metabolites, food products, herbal products) that have received comparatively little attention. We feel that now, especially given advances in determining protein-compound interactions, is an appropriate time to emphasize the diverse functions that drug transporters can perform.

Our primary goal in this issue is to shed light on the studies that demonstrate the diverse functions of drug transporters. Given the interest the pharmaceutical field generates, most research will focus on the different drugs and their affinities to these proteins, as well as the clinical implications this may have. However, increased attention on endogenous metabolites, which may serve as biomarkers for healthy and diseased states, and natural products, many of which can be purchased over the counter and used medicinally, begets research on the specific interactions between transporters and these small molecules. There are now a variety of in vivo, in vitro, and in silico tools and techniques that can be used to further probe the full extent of drug transporter function.

We welcome contributions in the following areas:

• Original research identifying new substrates/inhibitors of drug transporters or other related transporters. We are particularly interested in endogenous biomarkers, natural products, food components, and excipients.
• Original research showing clinical or physiological relevance of competition between drug and another non-pharmaceutical small molecule.
• Original research identifying important residues/pockets in transporter protein structures for transport/inhibition of small molecules.
• Review or mini-review describing recent advances in specificity relating to endogenous metabolites, herbs, or other non pharmaceutical products.
• Methods (experimental or computational) for confirming/predicting substrates/inhibitors of transporters.
• Commentaries from regulatory agencies describing the importance of non-pharmaceutical substrates/inhibitors.

Submit your idea

Impact

Frontiers in Pharmacology

Submit your idea

Impact