Mammalian ABC transporters in health and disease.

  title={Mammalian ABC transporters in health and disease.},
  author={Piet Borst and Ronald P.J. Oude Elferink},
  journal={Annual review of biochemistry},
The ATP-binding cassette (ABC) transporters are a family of large proteins in membranes and are able to transport a variety of compounds through membranes against steep concentration gradients at the cost of ATP hydrolysis. The available outline of the human genome contains 48 ABC genes; 16 of these have a known function and 14 are associated with a defined human disease. Major physiological functions of ABC transporters include the transport of lipids, bile salts, toxic compounds, and peptides… 

Figures from this paper

The ABC Transporters MDR1 and MRP2: Multiple Functions in Disposition of Xenobiotics and Drug Resistance

This work reviews the function of the human multidrug resistance protein MDR1, (P‐glycoprotein, ABCB1) and the multi-drug resistance protein MRP2 (ABCC2) and focuses on four topics namely structure and physiological functions of these transporters, substrates e.g., drugs, xenotoxins, and environmental toxicants including their conjugates, drug–drug interactions, and the role of chemosensitizers.


Drug-transporting proteins operate in pharmacokinetic and pharmacodynamic pathways, including pathways involved in both therapeutic and adverse effects (Figure 2–1).


Two unique roles of ABC transporters are studied in the liver and the heart, showing the diversity of ABCTransporters and the role they play in preventing cell toxicity and insight into ways to prevent cell toxicity through manipulation of ABC transport proteins.

ABC-transporters in the pig

The presented results provide for the first time detailed insight into the levels of expression and function of ABC transporters in pigs and confirm the good correlation between the kinetic data obtained from humans and pigs, and suggest that bioassays in pigs or with pig tissues may serve as an elegant model for kinetic studies with drugs and toxins affecting humans.

ABCG transporters: structure, substrate specificities and physiological roles

Evidence will be summarized suggesting that ABCG2 can also mediate the binding/transport of non-drug substrates, including free and conjugated steroids.

MRP class of human ATP binding cassette (ABC) transporters: historical background and new research directions

The historical background and discovery of the ATP-driven xenobiotic export pumps encoded by MRP genes, biological functions of ABC transporters belonging to the MRP class, and regulation of gene expression of MRPs by oxidative stress are addressed.

Structural snapshot of the cholesterol-transport ATP-binding cassette proteins 1.

A mechanistic model of ABC cholesterol transporters is proposed, addressing key structural features in the putative sterol translocation pathway on the transmembrane domains, and proposing a more relevant framework for mechanistic analysis of cholesterol-transport ABC proteins.

Transportomics: screening for substrates of ABC transporters in body fluids using vesicular transport assays

A new method to study the substrate spectrum of ABC transporters is described, and many new substrates of ABCC2 in urine are identified, including glucuronides of plant‐derived xenobiotics, a class of compounds to which humans are exposed on a daily basis.

Pharmacological functions of multidrug transporters: studies employing combination transporter knockout mice

P-gp and BCRP combination knockout mice enabled us to demonstrate that both multidrug transporters act in concert at the blood-brain barrier in restricting the brain penetration of the novel tyrosine kinase inhibitor anticancer drugs dasatinib and sorafenib.



The human ATP-binding cassette (ABC) transporter superfamily.

The current knowledge of the human ABC genes, their role in inherited disease, and understanding of the topology of these genes within the membrane are reviewed.

ABC transporters in lipid transport.

Multidrug ABC transporters from bacteria to man: an emerging hypothesis for the universality of molecular mechanism and function.

  • C. HrycynaM. Gottesman
  • Biology
    Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy
  • 1998

Membrane Transporters as Drug Targets

Detailed analysis of Renal Na+-Coupled Divalent Anion Transporters and molecular and Functional Characteristics of Cloned Human Organic Cation Transporter suggest that Bile Acids and Organic Anions are more likely to be transported than Organic Cations.

A family of drug transporters: the multidrug resistance-associated proteins.

Whether long-term inhibition of MRPs in humans can be tolerated (assuming that suitable inhibitors will be found) remains to be determined.

ABC proteins : from bacteria to man

The Transporter Associated with Antigen Processing (TAP): A Peptide Transport and Loading Complex Essential for Cellular Immune Responses The Sulphonylurea Receptor: an ABCC Transporter that Acts as an Ion Channel Regulator ABC-Transporters and Human Eye Disease Structure Function Analysis of CFTR.

Volume-regulated chloride channels associated with the human multidrug-resistance P-glycoprotein

It is reported here that expression of P-glycoprotein generates volume-regulated, ATP-dependent, chloride-selective channels, with properties similar to channels characterized previously in epithelial cells.

Role of metabolic enzymes and efflux transporters in the absorption of drugs from the small intestine.

  • H. SuzukiY. Sugiyama
  • Biology
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2000