What do drug transporters really do?

Nat Rev Drug Discov. 2015 Jan;14(1):29-44. doi: 10.1038/nrd4461. Epub 2014 Dec 5.


Potential drug-drug interactions mediated by the ATP-binding cassette (ABC) transporter and solute carrier (SLC) transporter families are of clinical and regulatory concern. However, the endogenous functions of these drug transporters are not well understood. Discussed here is evidence for the roles of ABC and SLC transporters in the handling of diverse substrates, including metabolites, antioxidants, signalling molecules, hormones, nutrients and neurotransmitters. It is suggested that these transporters may be part of a larger system of remote communication ('remote sensing and signalling') between cells, organs, body fluid compartments and perhaps even separate organisms. This broader view may help to clarify disease mechanisms, drug-metabolite interactions and drug effects relevant to diabetes, chronic kidney disease, metabolic syndrome, hypertension, gout, liver disease, neuropsychiatric disorders, inflammatory syndromes and organ injury, as well as prenatal and postnatal development.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / genetics
  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Biological Transport / physiology
  • Drug Interactions / physiology*
  • Humans
  • Membrane Transport Proteins / genetics
  • Membrane Transport Proteins / metabolism*
  • Organic Anion Transporters / genetics
  • Organic Anion Transporters / metabolism
  • Pharmaceutical Preparations / metabolism*


  • ATP-Binding Cassette Transporters
  • Membrane Transport Proteins
  • Organic Anion Transporters
  • Pharmaceutical Preparations