Regulatory pathways for ATP-binding cassette transport proteins in kidney proximal tubules

AAPS J. 2012 Dec;14(4):883-94. doi: 10.1208/s12248-012-9404-z. Epub 2012 Sep 8.


The ATP-binding cassette transport proteins (ABC transporters) represent important determinants of drug excretion. Protective or excretory tissues where these transporters mediate substrate efflux include the kidney proximal tubule. Regulation of the transport proteins in this tissue requires elaborate signaling pathways, including genetic, epigenetic, nuclear receptor mediated, posttranscriptional gene regulation involving microRNAs, and non-genomic (kinases) pathways triggered by hormones and/or growth factors. This review discusses current knowledge on regulatory pathways for ABC transporters in kidney proximal tubules, with a main focus on P-glycoprotein, multidrug resistance proteins 2 and 4, and breast cancer resistance protein. Insight in these processes is of importance because variations in transporter activity due to certain (disease) conditions could lead to significant changes in drug efficacy or toxicity.

Publication types

  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Drug-Related Side Effects and Adverse Reactions
  • Humans
  • Kidney Tubules, Proximal / metabolism*
  • Pharmaceutical Preparations / metabolism*
  • Signal Transduction


  • ATP-Binding Cassette Transporters
  • Pharmaceutical Preparations